A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
21-Amino-acid peptides produced by vascular endothelial cells and functioning as potent vasoconstrictors. The endothelin family consists of three members, ENDOTHELIN-1; ENDOTHELIN-2; and ENDOTHELIN-3. All three peptides contain 21 amino acids, but vary in amino acid composition. The three peptides produce vasoconstrictor and pressor responses in various parts of the body. However, the quantitative profiles of the pharmacological activities are considerably different among the three isopeptides.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
A 21-amino acid peptide that circulates in the plasma, but its source is not known. Endothelin-3 has been found in high concentrations in the brain and may regulate important functions in neurons and astrocytes, such as proliferation and development. It also is found throughout the gastrointestinal tract and in the lung and kidney. (N Eng J Med 1995;333(6):356-63)
A 21-amino acid peptide produced predominantly within the kidney and intestine, with smaller amounts produced in the myocardium, placenta, and uterus, but the cells of origin are not clear. Endothelin-2 has no unique physiologic functions, as compared with endothelin-1. (N Eng J Med 1995;333(6):356-63)
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
Venoms from SNAKES of the viperid family. They tend to be less toxic than elapid or hydrophid venoms and act mainly on the vascular system, interfering with coagulation and capillary membrane integrity and are highly cytotoxic. They contain large amounts of several enzymes, other factors, and some toxins.
A group of compounds that contain the structure SO2NH2.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
A sub-subclass of endopeptidases that depend on an ASPARTIC ACID residue for their activity.
Seven membered heterocyclic rings containing a NITROGEN atom.
Aryl CYCLOPENTANES that are a reduced (protonated) form of INDENES.
Peptides composed of between two and twelve amino acids.
Drugs used to cause constriction of the blood vessels.
A family of hexahydropyridines.
ENDOPEPTIDASES which use a metal such as ZINC in the catalytic mechanism.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.
The nonstriated involuntary muscle tissue of blood vessels.
Increased VASCULAR RESISTANCE in the PULMONARY CIRCULATION, usually secondary to HEART DISEASES or LUNG DISEASES.
Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.
The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM.
A free radical gas produced endogenously by a variety of mammalian cells, synthesized from ARGININE by NITRIC OXIDE SYNTHASE. Nitric oxide is one of the ENDOTHELIUM-DEPENDENT RELAXING FACTORS released by the vascular endothelium and mediates VASODILATION. It also inhibits platelet aggregation, induces disaggregation of aggregated platelets, and inhibits platelet adhesion to the vascular endothelium. Nitric oxide activates cytosolic GUANYLATE CYCLASE and thus elevates intracellular levels of CYCLIC GMP.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
The circulation of the BLOOD through the vessels of the KIDNEY.
The force that opposes the flow of BLOOD through a vascular bed. It is equal to the difference in BLOOD PRESSURE across the vascular bed divided by the CARDIAC OUTPUT.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Persistently high systemic arterial BLOOD PRESSURE. Based on multiple readings (BLOOD PRESSURE DETERMINATION), hypertension is currently defined as when SYSTOLIC PRESSURE is consistently greater than 140 mm Hg or when DIASTOLIC PRESSURE is consistently 90 mm Hg or more.
A strain of Rattus norvegicus used as a normotensive control for the spontaneous hypertensive rats (SHR).
Compounds that contain a 1-dimethylaminonaphthalene-5-sulfonyl group.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Drugs used to cause dilation of the blood vessels.
The short wide vessel arising from the conus arteriosus of the right ventricle and conveying unaerated blood to the lungs.
A process leading to shortening and/or development of tension in muscle tissue. Muscle contraction occurs by a sliding filament mechanism whereby actin filaments slide inward among the myosin filaments.
A family of 6-membered heterocyclic compounds occurring in nature in a wide variety of forms. They include several nucleic acid constituents (CYTOSINE; THYMINE; and URACIL) and form the basic structure of the barbiturates.
A potent natriuretic and vasodilatory peptide or mixture of different-sized low molecular weight PEPTIDES derived from a common precursor and secreted mainly by the HEART ATRIUM. All these peptides share a sequence of about 20 AMINO ACIDS.
Arteries which arise from the abdominal aorta and distribute to most of the intestines.
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
A strain of Rattus norvegicus with elevated blood pressure used as a model for studying hypertension and stroke.
The muscle tissue of the HEART. It is composed of striated, involuntary muscle cells (MYOCYTES, CARDIAC) connected to form the contractile pump to generate blood flow.
The veins and arteries of the HEART.
A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Proteins which contain carbohydrate groups attached covalently to the polypeptide chain. The protein moiety is the predominant group with the carbohydrate making up only a small percentage of the total weight.
The main trunk of the systemic arteries.
A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.
The smallest divisions of the arteries located between the muscular arteries and the capillaries.
Enzyme that is a major constituent of kidney brush-border membranes and is also present to a lesser degree in the brain and other tissues. It preferentially catalyzes cleavage at the amino group of hydrophobic residues of the B-chain of insulin as well as opioid peptides and other biologically active peptides. The enzyme is inhibited primarily by EDTA, phosphoramidon, and thiorphan and is reactivated by zinc. Neprilysin is identical to common acute lymphoblastic leukemia antigen (CALLA Antigen), an important marker in the diagnosis of human acute lymphocytic leukemia. There is no relationship with CALLA PLANT.
Azoles with an OXYGEN and a NITROGEN next to each other at the 1,2 positions, in contrast to OXAZOLES that have nitrogens at the 1,3 positions.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
An NADPH-dependent enzyme that catalyzes the conversion of L-ARGININE and OXYGEN to produce CITRULLINE and NITRIC OXIDE.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Mammalian pigment cells that produce MELANINS, pigments found mainly in the EPIDERMIS, but also in the eyes and the hair, by a process called melanogenesis. Coloration can be altered by the number of melanocytes or the amount of pigment produced and stored in the organelles called MELANOSOMES. The large non-mammalian melanin-containing cells are called MELANOPHORES.
The flow of BLOOD through or around an organ or region of the body.
A steroid metabolite that is the 11-deoxy derivative of CORTICOSTERONE and the 21-hydroxy derivative of PROGESTERONE.
Classic quantitative assay for detection of antigen-antibody reactions using a radioactively labeled substance (radioligand) either directly or indirectly to measure the binding of the unlabeled substance to a specific antibody or other receptor system. Non-immunogenic substances (e.g., haptens) can be measured if coupled to larger carrier proteins (e.g., bovine gamma-globulin or human serum albumin) capable of inducing antibody formation.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Any of various animals that constitute the family Suidae and comprise stout-bodied, short-legged omnivorous mammals with thick skin, usually covered with coarse bristles, a rather long mobile snout, and small tail. Included are the genera Babyrousa, Phacochoerus (wart hogs), and Sus, the latter containing the domestic pig (see SUS SCROFA).
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
Congenital MEGACOLON resulting from the absence of ganglion cells (aganglionosis) in a distal segment of the LARGE INTESTINE. The aganglionic segment is permanently contracted thus causing dilatation proximal to it. In most cases, the aganglionic segment is within the RECTUM and SIGMOID COLON.
Elements of limited time intervals, contributing to particular results or situations.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
The internal portion of the kidney, consisting of striated conical masses, the renal pyramids, whose bases are adjacent to the cortex and whose apices form prominent papillae projecting into the lumen of the minor calyces.
Genetically identical individuals developed from brother and sister matings which have been carried out for twenty or more generations or by parent x offspring matings carried out with certain restrictions. This also includes animals with a long history of closed colony breeding.
The neural systems which act on VASCULAR SMOOTH MUSCLE to control blood vessel diameter. The major neural control is through the sympathetic nervous system.
The portion of the descending aorta proceeding from the arch of the aorta and extending to the DIAPHRAGM, eventually connecting to the ABDOMINAL AORTA.
The circulation of the BLOOD through the LUNGS.
A competitive inhibitor of nitric oxide synthetase.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.
The vessels carrying blood away from the heart.
The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.
Unstable isotopes of iodine that decay or disintegrate emitting radiation. I atoms with atomic weights 117-139, except I 127, are radioactive iodine isotopes.
Part of the arm in humans and primates extending from the ELBOW to the WRIST.
Small circumscribed melanoses resembling, but differing histologically from, freckles. The concept includes senile lentigo ('liver spots') and nevoid lentigo (nevus spilus, lentigo simplex) and may also occur in association with multiple congenital defects or congenital syndromes (e.g., Peutz-Jeghers syndrome).
Treatment process involving the injection of fluid into an organ or tissue.
An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.
A nonsteroidal abortifacient agent that is effective in both the first and second trimesters of PREGNANCY.
Unstriated and unstriped muscle, one of the muscles of the internal organs, blood vessels, hair follicles, etc. Contractile elements are elongated, usually spindle-shaped cells with centrally located nuclei. Smooth muscle fibers are bound together into sheets or bundles by reticular fibers and frequently elastic nets are also abundant. (From Stedman, 25th ed)
An increase in the excretion of URINE. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
Antidiuretic hormones released by the NEUROHYPOPHYSIS of all vertebrates (structure varies with species) to regulate water balance and OSMOLARITY. In general, vasopressin is a nonapeptide consisting of a six-amino-acid ring with a cysteine 1 to cysteine 6 disulfide bridge or an octapeptide containing a CYSTINE. All mammals have arginine vasopressin except the pig with a lysine at position 8. Vasopressin, a vasoconstrictor, acts on the KIDNEY COLLECTING DUCTS to increase water reabsorption, increase blood volume and blood pressure.
An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
The domestic dog, Canis familiaris, comprising about 400 breeds, of the carnivore family CANIDAE. They are worldwide in distribution and live in association with people. (Walker's Mammals of the World, 5th ed, p1065)
Relatively complete absence of oxygen in one or more tissues.
The circulation of the BLOOD through the MICROVASCULAR NETWORK.
The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed)
Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.
A white crystal or crystalline powder used in BUFFERS; FERTILIZERS; and EXPLOSIVES. It can be used to replenish ELECTROLYTES and restore WATER-ELECTROLYTE BALANCE in treating HYPOKALEMIA.
Sodium chloride used in foods.
Derivatives of phosphatidic acids in which the phosphoric acid is bound in ester linkage to the hexahydroxy alcohol, myo-inositol. Complete hydrolysis yields 1 mole of glycerol, phosphoric acid, myo-inositol, and 2 moles of fatty acids.
The cartilaginous and membranous tube descending from the larynx and branching into the right and left main bronchi.
Sodium excretion by URINATION.
The hollow, muscular organ that maintains the circulation of the blood.
A highly specific (Leu-Leu) endopeptidase that generates ANGIOTENSIN I from its precursor ANGIOTENSINOGEN, leading to a cascade of reactions which elevate BLOOD PRESSURE and increase sodium retention by the kidney in the RENIN-ANGIOTENSIN SYSTEM. The enzyme was formerly listed as EC 3.4.99.19.
A neurotransmitter found at neuromuscular junctions, autonomic ganglia, parasympathetic effector junctions, a subset of sympathetic effector junctions, and at many sites in the central nervous system.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
The number of times the HEART VENTRICLES contract per unit of time, usually per minute.
The artery formed by the union of the right and left vertebral arteries; it runs from the lower to the upper border of the pons, where it bifurcates into the two posterior cerebral arteries.
A compound consisting of dark green crystals or crystalline powder, having a bronze-like luster. Solutions in water or alcohol have a deep blue color. Methylene blue is used as a bacteriologic stain and as an indicator. It inhibits GUANYLATE CYCLASE, and has been used to treat cyanide poisoning and to lower levels of METHEMOGLOBIN.
Either of the pair of organs occupying the cavity of the thorax that effect the aeration of the blood.
A class of drugs whose main indications are the treatment of hypertension and heart failure. They exert their hemodynamic effect mainly by inhibiting the renin-angiotensin system. They also modulate sympathetic nervous system activity and increase prostaglandin synthesis. They cause mainly vasodilation and mild natriuresis without affecting heart rate and contractility.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
A powerful vasodilator used in emergencies to lower blood pressure or to improve cardiac function. It is also an indicator for free sulfhydryl groups in proteins.
A region, of SOMITE development period, that contains a number of paired arches, each with a mesodermal core lined by ectoderm and endoderm on the two sides. In lower aquatic vertebrates, branchial arches develop into GILLS. In higher vertebrates, the arches forms outpouchings and develop into structures of the head and neck. Separating the arches are the branchial clefts or grooves.
A syndrome characterized by the clinical triad of advanced chronic liver disease, pulmonary vascular dilatations, and reduced arterial oxygenation (HYPOXEMIA) in the absence of intrinsic cardiopulmonary disease. This syndrome is common in the patients with LIVER CIRRHOSIS or portal hypertension (HYPERTENSION, PORTAL).
Cell surface proteins that bind signalling molecules external to the cell with high affinity and convert this extracellular event into one or more intracellular signals that alter the behavior of the target cell (From Alberts, Molecular Biology of the Cell, 2nd ed, pp693-5). Cell surface receptors, unlike enzymes, do not chemically alter their ligands.
A heterogeneous condition in which the heart is unable to pump out sufficient blood to meet the metabolic need of the body. Heart failure can be caused by structural defects, functional abnormalities (VENTRICULAR DYSFUNCTION), or a sudden overload beyond its capacity. Chronic heart failure is more common than acute heart failure which results from sudden insult to cardiac function, such as MYOCARDIAL INFARCTION.
Phosphoric acid esters of inositol. They include mono- and polyphosphoric acid esters, with the exception of inositol hexaphosphate which is PHYTIC ACID.
Two ganglionated neural plexuses in the gut wall which form one of the three major divisions of the autonomic nervous system. The enteric nervous system innervates the gastrointestinal tract, the pancreas, and the gallbladder. It contains sensory neurons, interneurons, and motor neurons. Thus the circuitry can autonomously sense the tension and the chemical environment in the gut and regulate blood vessel tone, motility, secretions, and fluid transport. The system is itself governed by the central nervous system and receives both parasympathetic and sympathetic innervation. (From Kandel, Schwartz, and Jessel, Principles of Neural Science, 3d ed, p766)
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
Contractile activity of the MYOCARDIUM.
A non-steroidal anti-inflammatory agent (NSAID) that inhibits the enzyme cyclooxygenase necessary for the formation of prostaglandins and other autacoids. It also inhibits the motility of polymorphonuclear leukocytes.
The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.
The predominant form of mammalian antidiuretic hormone. It is a nonapeptide containing an ARGININE at residue 8 and two disulfide-linked cysteines at residues of 1 and 6. Arg-vasopressin is used to treat DIABETES INSIPIDUS or to improve vasomotor tone and BLOOD PRESSURE.
A pyrrolizidine alkaloid and a toxic plant constituent that poisons livestock and humans through the ingestion of contaminated grains and other foods. The alkaloid causes pulmonary artery hypertension, right ventricular hypertrophy, and pathological changes in the pulmonary vasculature. Significant attenuation of the cardiopulmonary changes are noted after oral magnesium treatment.
Regional infusion of drugs via an arterial catheter. Often a pump is used to impel the drug through the catheter. Used in therapy of cancer, upper gastrointestinal hemorrhage, infection, and peripheral vascular disease.
The rate dynamics in chemical or physical systems.
A prostaglandin that is a powerful vasodilator and inhibits platelet aggregation. It is biosynthesized enzymatically from PROSTAGLANDIN ENDOPEROXIDES in human vascular tissue. The sodium salt has been also used to treat primary pulmonary hypertension (HYPERTENSION, PULMONARY).
General increase in bulk of a part or organ due to CELL ENLARGEMENT and accumulation of FLUIDS AND SECRETIONS, not due to tumor formation, nor to an increase in the number of cells (HYPERPLASIA).
Compounds which inhibit or antagonize biosynthesis or actions of proteases (ENDOPEPTIDASES).
Rapidly decreasing response to a drug or physiologically active agent after administration of a few doses. In immunology, it is the rapid immunization against the effect of toxic doses of an extract or serum by previous injection of small doses. (Dorland, 28th ed)
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
The two longitudinal ridges along the PRIMITIVE STREAK appearing near the end of GASTRULATION during development of nervous system (NEURULATION). The ridges are formed by folding of NEURAL PLATE. Between the ridges is a neural groove which deepens as the fold become elevated. When the folds meet at midline, the groove becomes a closed tube, the NEURAL TUBE.
The circulation of blood through the CORONARY VESSELS of the HEART.
A CALCIUM-dependent, constitutively-expressed form of nitric oxide synthase found primarily in ENDOTHELIAL CELLS.
A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.
A method of non-invasive, continuous measurement of MICROCIRCULATION. The technique is based on the values of the DOPPLER EFFECT of low-power laser light scattered randomly by static structures and moving tissue particulates.
A tetradecapeptide originally obtained from the skins of toads Bombina bombina and B. variegata. It is also an endogenous neurotransmitter in many animals including mammals. Bombesin affects vascular and other smooth muscle, gastric secretion, and renal circulation and function.
A condition associated with VENTRICULAR SEPTAL DEFECT and other congenital heart defects that allow the mixing of pulmonary and systemic circulation, increase blood flow into the lung, and subsequent responses to low oxygen in blood. This complex is characterized by progressive PULMONARY HYPERTENSION; HYPERTROPHY of the RIGHT VENTRICLE; CYANOSIS; and ERYTHROCYTOSIS.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
A cluster of convoluted capillaries beginning at each nephric tubule in the kidney and held together by connective tissue.
An essential amino acid that is physiologically active in the L-form.
The thin membranous structure supporting the adjoining glomerular capillaries. It is composed of GLOMERULAR MESANGIAL CELLS and their EXTRACELLULAR MATRIX.
An inhibitor of nitric oxide synthetase which has been shown to prevent glutamate toxicity. Nitroarginine has been experimentally tested for its ability to prevent ammonia toxicity and ammonia-induced alterations in brain energy and ammonia metabolites. (Neurochem Res 1995:200(4):451-6)
Detection of RNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.

Role of endothelin in the increased vascular tone of patients with essential hypertension. (1/3445)

We investigated the possible role of endothelin in the increased vasoconstrictor tone of hypertensive patients using antagonists of endothelin receptors. Forearm blood flow (FBF) responses (strain-gauge plethysmography) to intraarterial infusion of blockers of endothelin-A (ETA) (BQ-123) and endothelin-B (ETB) (BQ-788) receptors, separately and in combination, were measured in hypertensive patients and normotensive control subjects. In healthy subjects, BQ-123 alone or in combination with BQ-788 did not significantly modify FBF (P=0.78 and P=0.63, respectively). In hypertensive patients, in contrast, BQ-123 increased FBF by 33+/-7% (P<0.001 versus baseline), and the combination of BQ-123 and BQ-788 resulted in a greater vasodilator response (63+/-12%; P=0.006 versus BQ-123 alone in the same subjects). BQ-788 produced a divergent vasoactive effect in the two groups, with a decrease of FBF (17+/-5%; P=0.004 versus baseline) in control subjects and transient vasodilation (15+/-7% after 20 minutes) in hypertensive patients (P<0.001, hypertensives versus controls). The vasoconstrictor response to endothelin-1 was slightly higher (P=0.04) in hypertensive patients (46+/-4%) than in control subjects (32+/-4%). Our data indicate that patients with essential hypertension have increased vascular endothelin activity, which may be of pathophysiological relevance to their increased vascular tone. In these patients, nonselective ETA and ETB blockade seems to produce a greater vasodilator effect than selective ETA blockade.  (+info)

Different contributions of endothelin-A and endothelin-B receptors in the pathogenesis of deoxycorticosterone acetate-salt-induced hypertension in rats. (2/3445)

We investigated the involvement of actions mediated by endothelin-A (ETA) and endothelin-B (ETB) receptors in the pathogenesis of deoxycorticosterone acetate (DOCA)-salt-induced hypertension in rats. Two weeks after the start of DOCA-salt treatment, rats were given ABT-627 (10 [mg/kg]/d), a selective ETA receptor antagonist; A-192621 (30 [mg/kg]/d), a selective ETB receptor antagonist; or their vehicle for 2 weeks. Uninephrectomized rats without DOCA-salt treatment served as controls. Treatment with DOCA and salt for 2 weeks led to a mild but significant hypertension; in vehicle-treated DOCA-salt rats, systolic blood pressure increased markedly after 3 to 4 weeks. Daily administration of ABT-627 for 2 weeks almost abolished any further increases in blood pressure, whereas A-192621 did not affect the development of DOCA-salt-induced hypertension. When the degree of vascular hypertrophy of the aorta was histochemically evaluated at 4 weeks, there were significant increases in wall thickness, wall area, and wall-to-lumen ratio in vehicle-treated DOCA-salt rats compared with uninephrectomized control rats. The development of vascular hypertrophy was markedly suppressed by ABT-627. In contrast, treatment with A-192621 significantly exaggerated these vascular changes. In vehicle-treated DOCA-salt rats, renal blood flow and creatinine clearance decreased, and urinary excretion of protein, blood urea nitrogen, fractional excretion of sodium, and urinary N-acetyl-beta-glucosaminidase activity increased. Such damage was overcome by treatment with ABT-627 but not with A-192621; indeed, the latter agent led to worsening of the renal dysfunction. Histopathologic examination of the kidney in vehicle-treated DOCA-salt rats revealed tubular dilatation and atrophy as well as thickening of small arteries. Such damage was reduced in animals given ABT-627, whereas more severe histopathologic changes were observed in A-192621-treated animals. These results strongly support the view that ETA receptor-mediated action plays an important role in the pathogenesis of DOCA-salt-induced hypertension. On the other hand, it seems likely that the ETB receptor-mediated action protects against vascular and renal injuries in this model of hypertension. A selective ETA receptor antagonist is likely to be useful for treatment of subjects with mineralocorticoid-dependent hypertension, whereas ETB-selective antagonism alone is detrimental to such cases.  (+info)

Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat-1 fibroblasts stably expressing alpha1d-adrenoceptors. (3/3445)

In rat-1 fibroblasts stably expressing alpha1d-adrenoceptors BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil decreased basal [Ca2+]i. WB 4101 induced a very small effect on this parameter but when added before the other antagonists it blocked their effect. All these agents inhibited the action of norepinephrine. Phorbol myristate acetate also blocked the effect of norepinephrine and decreased basal [Ca2+]i. Staurosporine inhibited these effects of the phorbol ester. Our results suggest that: (1) alpha1d-adrenoceptors exhibit spontaneous ligand-independent activity, (2) BMY 7378, phentolamine, chloroethylclonidine and 5-methyl urapidil act as inverse agonists and (3) protein kinase C activation blocks spontaneous and agonist-stimulated alpha1d-adrenoceptor activity.  (+info)

Endogenous plasma endothelin concentrations and coronary circulation in patients with mild dilated cardiomyopathy. (4/3445)

OBJECTIVE: To determine whether increased plasma concentrations of endothelin-1 (ET-1) and big endothelin (BET) play a role in the regulation of coronary circulation in patients with idiopathic dilated cardiomyopathy (IDCM). SETTING: Tertiary referral centre for cardiac diseases. PATIENTS: Fourteen patients (eight male/six female; mean (SD) age 59 (9) years) with IDCM (ejection fraction 36 (9)%) and five normotensive subjects (two male/three female; age 52 (7) years) serving as controls were studied. METHODS: Functional status was classified according to New York Heart Association (NYHA) class. Endogenous ET-1 and BET plasma concentrations from the aorta and the coronary sinus were determined by radioimmunoassay. Coronary blood flow, using the inert chromatographic argon method, myocardial oxygen consumption, and coronary sinus oxygen content under basal conditions were determined. RESULTS: In the aorta, mean (SD) concentrations of ET-1 (IDCM 0.76 (0.25) v controls 0.31 (0.06) fmol/ml; p = 0.002) and BET (IDCM 3.58 (1.06) v controls 2.11 (0.58) fmol/ml; p = 0.014) were increased in patients with IDCM. Aortic ET-1 concentrations correlated positively with NYHA class (r = 0. 731; p < 0.001), myocardial oxygen consumption (r = 0.749; p < 0. 001), and coronary blood flow (r = 0.645; p = 0.003), but inversely with coronary sinus oxygen content (r = -0.633; p = 0.004), which was significantly decreased in IDCM patients (IDCM 4.68 (1.05) v controls 6.70 (1.06) vol%; p = 0.003). CONCLUSIONS: The coronary circulation in patients with IDCM is exposed to an increased endothelin load. ET-1 concentrations correlate with functional deterioration. A decrease of the coronary sinus content of oxygen suggests a mismatch between coronary blood flow and metabolic demand. Thus, ET-1 might be a marker of a disequilibrium between myocardial oxygen demand and coronary blood flow in IDCM.  (+info)

Nitric oxide modulates endothelin 1-induced Ca2+ mobilization and cytoskeletal F-actin filaments in human cerebromicrovascular endothelial cells. (5/3445)

A functional interrelation between nitric oxide (NO), the endothelial-derived vasodilating factor, and endothelin 1 (ET-1), the potent vasoconstrictive peptide, was investigated in microvascular endothelium of human brain. Nor-1 dose-dependently decreased the ET-1-stimulated mobilization of Ca2+. This response was mimicked with cGMP and abrogated by inhibitors of guanylyl cyclase or cGMP-dependent protein kinase G. These findings indicate that NO and ET-1 interactions involved in modulation of intracellular Ca2+ are mediated by cGMP/protein kinase G. In addition, Nor-1-mediated effects were associated with rearrangements of cytoskeleton F-actin filaments. The results suggest mechanisms by which NO-ET-1 interactions may contribute to regulation of microvascular function.  (+info)

Endogenous endothelin-1 depresses left ventricular systolic and diastolic performance in congestive heart failure. (6/3445)

Endothelin-1 (ET-1) is a positive inotrope in normal hearts; however, the direct cardiac effects of endogenous ET-1 in congestive heart failure (CHF) are unknown. We evaluated the cardiac responses to endogenous ET-1 using an ETA and ETB receptor blocker (L-754,142) in seven conscious dogs before and after pacing-induced CHF. Before CHF, when the plasma ET-1 was 7.3 +/- 1.7 fmol/ml, L-754,142 caused no significant alterations in heart rate, left ventricular (LV) end-systolic pressure, total systemic resistance, and the time constant of LV relaxation (tau). LV contractile performance, measured by the slopes of LV pressure (P)-volume (V) relation (EES), dP/dtmax-end-diastolic V relation (dE/dtmax), and stroke work-end-diastolic V relation, was also unaffected. After CHF, when the plasma ET-1 was significantly increased to 14.1 +/- 3.0 fmol/ml (p <.05), L-754,142 produced a significant decreases in LV end-systolic pressure (101 +/- 11 versus 93 +/- 8 mm Hg) and total systemic resistance (0.084 +/- 0.022 versus 0.065 +/- 0.15 mm Hg/ml/min). The tau (42 +/- 12 versus 38 +/- 10 ms), mean left atrial P (22 +/- 5 versus 18 +/- 4 mm Hg) (p <.05), and minimum LVP were also significantly decreased. After CHF, the slopes of P-V relations, EES (3.4 +/- 0.4 versus 4.8 +/- 0.8 mm Hg/ml), dE/dtmax (42.4 +/- 7.8 versus 50.0 +/- 7.8 mm Hg/s/ml), and stroke work-end-diastolic V relation (58.1 +/- 3.3 versus 72.4 +/- 5.2 mm Hg) (p <.05) all increased after L-754,142, indicating enhanced contractility. Before CHF, low levels of endogenous ET-1 have little cardiac effect. However, after CHF, elevated endogenous ET-1 produces arterial vasoconstriction, slows LV relaxation, and depresses LV contractile performance. Thus, elevated endogenous ET-1 may contribute to the functional impairment in CHF in this canine model.  (+info)

Relaxation of endothelin-1-induced pulmonary arterial constriction by niflumic acid and NPPB: mechanism(s) independent of chloride channel block. (7/3445)

We investigated the effects of the Cl- channel blockers niflumic acid, 5-nitro-2-(3-phenylpropylamino)-benzoic acid (NPPB) and 4, 4'-diisothiocyanatostilbene-2,2'-disulphonic acid (DIDS) on endothelin-1 (ET-1)-induced constriction of rat small pulmonary arteries (diameter 100-400 microm) in vitro, following endothelium removal. ET-1 (30 nM) induced a sustained constriction of rat pulmonary arteries in physiological salt solution. Arteries preconstricted with ET-1 were relaxed by niflumic acid (IC50: 35.8 microM) and NPPB (IC50: 21.1 microM) in a reversible and concentration-dependent manner. However, at concentrations known to block Ca++-activated Cl- channels, DIDS (+info)

Endothelin up-regulation and localization following renal ischemia and reperfusion. (8/3445)

BACKGROUND: Endothelin (ET), a potent vasoconstrictor, is known to play a role in ischemic acute renal failure. Although preproET-1 (ppET-1) mRNA is known to be up-regulated following ischemia/reperfusion injury, it has not been determined which component of the injury (ischemia or reperfusion) leads to initial gene up-regulation. Likewise, although ET-1 peptide expression has been localized in the normal kidney, its expression pattern in the ischemic kidney has not been determined. Therefore, the purpose of this study was twofold: (a) to determine whether ischemia alone or ischemia plus reperfusion is required for the up-regulation of ppET-1 mRNA to occur, and (b) to localize ET-1 peptide expression following ischemia in the rat kidney to clarify better the role of ET in the pathophysiology of ischemia-induced acute renal failure. METHODS: Male Lewis rats underwent clamping of the right renal vascular pedicle for either 30 minutes of ischemia (group 1), 60 minutes of ischemia (group 2), 30 minutes of ischemia followed by 30 minutes of reperfusion (group 3), or 60 minutes of ischemia followed by three hours of reperfusion (group 4). The contralateral kidney acted as a control. ppET-1 mRNA up-regulation and ET-1 peptide expression were examined using the reverse transcription-polymerase chain reaction and immunohistochemistry, respectively. RESULTS: Reverse transcription-polymerase chain reaction yielded a control (nonischemic) value of 0.6 +/- 0.2 densitometric units (DU) of ppET-1 mRNA in the kidney. Group 1 levels (30 min of ischemia alone) were 1.8 +/- 0.4 DU, a threefold increase (P < 0.05). Group 2 levels (60 min of ischemia alone) increased almost six times above baseline, 3.5 +/- 0.2 DU (P < 0.01), whereas both group 3 and group 4 (ischemia plus reperfusion) did not experience any further significant increases in mRNA levels (1.9 +/- 0.4 DU and 2.8 +/- 0.6 DU, respectively) beyond levels in group 1 or 2 animals subjected to similar ischemic periods. ET-1 peptide expression in the ischemic kidneys was significantly increased over controls and was clearly localized to the endothelium of the peritubular capillary network of the kidney. CONCLUSIONS: Initial ET-1 gene up-regulation in the kidney occurs secondary to ischemia, but reperfusion most likely contributes to sustaining this up-regulation. The marked increase of ET-1 in the peritubular capillary network suggests that ET-induced vasoconstriction may have a pathophysiological role in ischemic acute tubular necrosis.  (+info)

Since its discovery in 1988 the powerful vasoconstrictor endothelin-1 (ET-1) has been widely implicated in the pathophysiology of chronic kidney disease (CKD) as well as the cardiovascular disease with which it is associated. ET receptor antagonists have favourable effects in experimental models of these conditions and orally acting antagonists are now licensed for the treatment of pulmonary arterial hypertension. However, there is a paucity of human data regarding the role of ET-1 in CKD. In this thesis, I have therefore explored the utility of ET-1 as a biomarker in CKD, and, using selective ET receptor antagonists, the beneficial renal and cardiovascular effects of ET receptor antagonism in CKD. I have shown that as glomerular filtration rate (GFR) declines plasma ET-1 increases linearly whereas urinary ET-1 shows an exponential increase. Furthermore, urinary ET-1 may be a useful marker of disease activity in patients with lupus nephritis. Its levels are high in those with biopsy-proven ...
The literature shows an increase in endothelin-1 with increased levels of erythrocytes. There are also indications that inflammation and elevated endothelin-1 levels interact with erythropoiesis. In this study, the association of erythrocytes and endothelin-1 in women of different ethnicities was investigated. Blood pressure, vascular resistance, and C-reactive protein (P = 0.09) were significantly higher in the African women (n = 102) compared to the Caucasian women (n = 115), while arterial compliance was significantly lower in the African women with no significant differences for endothelin-1. In single, partial, and multiple regression analyses, there was a significant positive correlation between the red blood cell count and log endothelin-1 in the Caucasians while in the Africans there was a weak negative correlation. This is an indication that endothelin-1 might interfere with erythrocyte production in Africans with higher levels of inflammation ...
TY - JOUR. T1 - Changes of endothelin-1 and big endothelin-1 levels and action potential duration during myocardial ischemia-reperfusion in dogs with and without ventricular fibrillation. AU - Vágó, Hajnalka. AU - Soós, Pál. AU - Zima, Endre. AU - Gellér, László. AU - Keltai, Katalin. AU - Róka, Attila. AU - Kékesi, Violetta. AU - Juhász-Nagy, Alexander. AU - Merkely, Béla. PY - 2004/11. Y1 - 2004/11. N2 - Myocardial ischemia-reperfusion is associated with increased production of endothelin-1 (ET-1). Moreover, exogenous ET-1 has arrhythmogenic properties. Our aim was to investigate the correlation between endogenous ET-1, big ET-1 levels and epicardial monophasic action potential duration during myocardial ischemia-reperfusion in anesthetized dogs. Thirty-minute myocardial ischemia was followed by a 90-minute reperfusion period in 18 mongrel dogs. The total incidence of ventricular fibrillation (VF) during ischemia and reperfusion was 11.1% and 33.3%, respectively. During ischemia, ...
Hypertension is largely attributed to abnormal renal sodium handling; however, a growing body of evidence now suggests that primary abnormalities in vessels can also cause aberrations in blood pressure. Very often, the source of the abnormality resides in the endothelial cells that regulate the functional state of the entire vessel, and this knowledge has directed our search for new diagnostic and therapeutic targets. To date, the role of transcriptional mechanisms in blood pressure regulation is poorly characterized. In this study, we found that E2F2, a transcription factor involved in cell-cycle control, regulates blood pressure by modulating vessel contractility. This previously unknown function of E2F2 evolves from the unique role of the molecule in endothelial cells: suppression of endothelin-converting enzyme 1 (ECE-1). ECE-1 converts the inactive precursor molecule big endothelin-1 into the potent vasoconstrictor endothelin-1, and genetic deletion of E2F2 in mice was associated with both ...
Milk protein-derived peptides with angiotensin-converting enzyme (ACE) inhibitory activity can reduce blood pressure in hypertensive subjects. The lactokinin Ala-Leu-Pro-Met-His-Ile-Arg (ALPMHIR) is an ACE-inhibitory peptide released by tryptic digestion from the milk protein beta-lactoglobulin. Its ACE-inhibitory activity is 100 times lower than that of captopril. The latter is known to inhibit the release of the vasoconstrictor endothelin-1 (ET-1) by endothelial cells. The effects of ALPMHIR on the endothelium are currently unknown. In this study, the influence of ALPMHIR on release of ET-1 by endothelial cells was investigated. The basal ET-1 release of the cells was reduced by 29% (p,0.01) in the presence of 1 mM ALPMHIR, compared to 42% (p,0.01) for 0.1 mM captopril. Addition of 10 U/ml thrombin to the incubation medium increased the release of ET-1 by 66% (p,0.01). Co-incubation of 10 U/ml thrombin with 1 microM captopril or with 0.1 mM ALPMHIR inhibited the stimulated ET-1 release by 45% ...
TY - JOUR. T1 - TRAF3IP2 mediates high glucose-induced endothelin-1 production as well as endothelin-1-induced inflammation in endothelial cells. AU - Padilla, Jaume. AU - Carpenter, Andrea J. AU - Das, Nitin A. AU - Kandikattu, Hemanth Kumar. AU - López-Ongil, Susana. AU - Martinez-Lemus, Luis A.. AU - Siebenlist, Ulrich. AU - DeMarco, Vincent G.. AU - Chandrasekar, Bysani. PY - 2018/1/1. Y1 - 2018/1/1. N2 - Hy-perglycemia-induced production of endothelin (ET)-1 is a hallmark of endothelial dysfunction in diabetes. Although the detrimental vascular effects of increased ET-1 are well known, the molecular mechanisms regulating endothelial synthesis of ET-1 in the setting of diabetes remain largely unidentified. Here, we show that adapter molecule TRAF3 interacting protein 2 (TRAF3IP2) mediates high glucose-induced ET-1 production in endothelial cells and ET-1-mediated endothelial cell inflammation. Specifically, we found that high glucose upregulated TRAF3IP2 in human aortic endothelial cells, ...
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Increased basal ET-1 release by NOS inhibitor was observed in only 2 of 9 studies with static cultures36,37 (Figure). Furthermore, in these 2 studies, the increased ET-1 release was determined after prolonged incubation with NOS inhibitor (ie, 637 and 24 hours36). Thus, the observed ET-1 release36,37 is not reflective of possible acute negative regulation of ET-1 release by NO.. Other studies failed to demonstrate increased ET-1 release after extended incubation (3-24 hours) with NOS inhibitor27,35,38-41 (Figure). Importantly, the general inability of NOS inhibitor to increase ET-1 release does not seem to be because of the failure of NOS inhibitor to decrease NO because NOS inhibitor for 8 hours decreased basal NO by 75% but did not increase ET-1 release41 (Figure; Figure S1).. The effect of NO inactivation on basal ET-1 release was also examined with oxyhemoglobin, which binds NO38,39,42,43 (Figure). Although exposure to oxyhemoglobin for 1 to 24 hours increased ET-1 release, it is likely that ...
Krishnaswamy and colleagues outline several mechanisms by which mast cells might contribute to plaque inflammation and rupture. Further work is needed to establish a direct role for mast cells in plaque instability. The hypothesis that plaque behavior could be favorably altered by preventing mast-cell degranulation or by inhibiting mast-cell proteases is intriguing but as yet unproven. Drs. Doherty and McMillen point out the several proatherogenic properties of endothelin-1. The work by Zeiher and coworkers (1) suggests that endothelin-1 is involved in the pathogenesis of acute coronary syndromes. However, evidence for endothelin-1 as an important determinant of plaque vulnerability and rupture is yet to come. With the introduction of endothelin-1 antagonists, an opportunity exists to further explore the role of endothelin-1 in the behavior of atherosclerotic plaques. If endothelin-1 antagonists do reduce coronary events, a central role for endothelin in promoting plaque instability could then ...
The effects of intravenous endothelin-1 (ET-1) on the ventilatory response to hypoxia were studied in healthy humans. Nine volunteers were each exposed twice to 4 hr eucapnic hypoxia. They received a continuous infusion of ET-1 during the ET-1 protocol and an infusion of saline during the control protocol. Plasma ET-1 levels and an index of ventilation were measured regularly. Hypoxia caused a rise in plasma ET-1 in the control protocol. Hypoxia also caused the index of ventilation to increase in both protocols, and this increase was greater in the ET-1 protocol than in the control protocol. These results are consistent with the hypothesis that ET-1 plays a role in controlling the ventilatory response to hypoxia in man.
TY - JOUR. T1 - Endothelin-1 critically influences cardiac function via superoxide-MMP9 cascade. AU - Hathaway, Catherine K.. AU - Grant, Ruriko. AU - Hagaman, John R.. AU - Hiller, Sylvia. AU - Li, Feng. AU - Xu, Longquan. AU - Chang, Albert S.. AU - Madden, Victoria J.. AU - Bagnell, C. Robert. AU - Rojas, Mauricio. AU - Kim, Hyung Suk. AU - Wu, Bingruo. AU - Zhou, Bin. AU - Smithies, Oliver. AU - Kakoki, Masao. PY - 2015/4/21. Y1 - 2015/4/21. N2 - We have generated low-expressing and high-expressing endothelin-1 genes (L and H) and have bred mice with four levels of expression: L/L, ∼20%; L/+, ∼65%; +/+ (wild type), 100%; and H/+, ∼350%. The hypomorphic L allele can be spatiotemporally switched to the hypermorphic H allele by Cre-loxP recombination. Young adult L/L and L/+ mice have dilated cardiomyopathy, hypertension, and increased plasma volumes, together with increased ventricular superoxide levels, increased matrix metalloproteinase 9 (Mmp9) expression, and reduced ventricular ...
Characterization of canine pericardial fluid endothelin-1 levels.: Recently, extremely high concentrations of endothelin-1 (ET-1) were detected in the pericardi
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Semantic Scholar extracted view of Increased sensitivity to endothelin-1 in spontaneously hypertensive rats is closely related to resting membrane potential by Tomohisa Ishikawa et al.
Aims: Contrast media-induced nephropathy (CIN) is associated with increased morbidity and mortality. The renal endothelin system has been associated with disease progression of various acute and chronic renal diseases. However, robust data coming from adequately powered prospective clinical studies analyzing the short and long-term impacts of the renal ET system in patients with CIN are missing so far. We thus performed a prospective study addressing this topic. Main methods: We included 327 patients with diabetes or renal impairment undergoing coronary angiography. Blood and spot urine were collected before and 24 h after contrast media (CM) application. Patients were followed for 90 days for major clinical events like need for dialysis, unplanned rehospitalization or death. Key findings: The concentration of ET-1 and the urinary ET-1/creatinine ratio decreased in spot urine after CM application (ET-1 concentration: 0.91 +/- 1.23pg/ml versus 0.63 +/- 1.03pg/ml, p,0.001; ET-1/creatinine ratio: ...
These findings demonstrate that acute exposure to vehicular source air pollutants results in upregulation of circulating and vascular factors associated with progression of atherosclerosis, mediated in part through activation of ET-1-ET(A) receptor pathways.
Peptides , Cyclic Peptides , Disulfide Cyclized Peptides , Big Endothelin-1 (1-38), human; Big Endothelin-1 (1-38) is precursor of endothelin 1. Big endothelin-1 is cleaved to yield endothelin-1 via the activity of an endothelin-converting enzyme (ECE). Big Endothelin-1 can be hydrolyzed by chymase to generate endothelin 1 (1-21) in vitro. Endothelins are endothelium-derived vasoconstrictor peptides.; CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRS (Disulfide bridge: 1-15 and 3-11); H-Cys-Ser-Cys-Ser-Ser-Leu-Met-Asp-Lys-Glu-Cys-Val-Tyr-Phe-Cys-His-Leu-Asp-Ile-Ile-Trp-Val-Asn-Thr-Pro-Glu-His-Val-Val-Pro-Tyr-Gly-Leu-Gly-Ser-Pro-Arg-Ser-OH (Disulfide bridge: 1-15 and 3-11)
Low levels of plasma endothelin-1 in patients with retinitis pigmentosa Hiroshi Ohguro1, Yukihiko Mashima2, Mitsuru Nakazawa31Department of Ophthalmology, Sapporo Medical University School of Medicine, 2Department of Ophthalmology, Keio University School of Medicine, 3Department of Ophthalmology, Hirosaki University School of Medicine, JapanPurpose: The aim of this study was to elucidate the role of endothelin-1 (ET-1) in the pathophysiology of retinitis pigmentosa (RP).Methods: Plasma ET-1 levels and ophthalmic features in 50 RP patients were compared with those in 20 healthy-eye control subjects. Plasma ET-1 concentrations were determined using a commercially available enzyme-linked immunosorbent assay kit.Results: Mean plasma ET-1 levels of RP patients (1.88 ± 0.56 pg/mL) were significantly lower than those of control subjects (2.30 ± 0.30 pg/mL, Mann-Whitney’s U test; P < 0.01). However, ET-1 concentrations varied markedly in each patient. Among RP patients, a significant
TY - JOUR. T1 - Identification of endothelin-1 in the pathophysiology of metastatic adenocarcinoma of the prostate. AU - Nelson, J. B.. AU - Hedican, S. P.. AU - George, D. J.. AU - Reddi, A Hari. AU - Piantadosi, S.. AU - Eisenberger, M. A.. AU - Simons, J. W.. PY - 1995. Y1 - 1995. N2 - Prostate cancer is the second most common cause of death from cancer in U.S. men, and advanced, hormone-refractory disease is characterized by painful osteoblastic bone metastases. Endothelin-1, more commonly known as a potent vasoconstrictor, is a normal ejaculate protein that also stimulates osteoblasts. We show here that plasma immunoreactive endothelin concentrations are significantly elevated in men with metastatic prostate cancer and that every human prostate cancer cell line tested produces endothelin-1 messenger RNA and secretes immunoreactive endothelin. Exogenous endothelin-1 is a prostate cancer mitogen in vitro and increases alkaline phosphatase activity in new bone formation, indicating that ...
The present study shows that antagonism of endogenous endothelin-1 produces marked decreases in aortic and ventricular systolic pressures in hypertensive dogs. These decreases persist for at least 1 hour after discontinuation of the drug, which could be explained by the 3-hour half-life of bosentan (M. Clozel, personal communication, 1994). Although systemic vascular resistances were not determined, it is likely that these changes resulted from peripheral vasodilation rather than from a depression in myocardial function. A significant decrease in filling pressures, as assessed by LVEDP and LAP, was observed. Both end-diastolic and systolic volumes also tended to decrease. Finally, indexes of cardiac performance, such as peak (+)dP/dt or myocardial segmental shortening, remained unchanged. The decrease in mean AOP in hypertensive dogs, which averaged 38 mm Hg, clearly suggests that endogenous endothelin-1 might play a role in the pathogenesis of renal hypertension. This role of endothelin-1 is ...
Glyceraldehyde-3-phosphate dehydrogenase (GAPDH) plays a key role in vascular homeostasis by modulating expression levels of the vasoconstrictor endothelin-1 (ET-1). Elevated ET-1 levels are associated with vascular diseases, and ET-1 expression is tightly regulated via GAPDH-mediated destabilization of its mRNA. Recent studies suggest GAPDH binding of adenine-uridine rich elements (AREs) in the 3-untranslated region (3-UTR) of the ET-1 gene leads to decreased mRNA stability. However, structural and mechanistic details underlying the GAPDH-mediated control of ET-1 expression are lacking. We sought to elucidate the structural and mechanistic details for the GAPDH-induced destabilization of ET-1 mRNA via electrophoretic mobility shift assay (EMSA), isothermal titration calorimetry (ITC), and x-ray crystallography. To identify specific GAPDH binding sequences, we constructed short RNA transcripts of the putative mRNA binding region. Utilizing ITC and EMSA, we obtained dissociation constants. We ...
Endothelins are among the most potent vasoconstrictor proteins known. Overexpression of endothelins contributes to hypertension and heart disease. Three isoforms are known, each containing 21 amino acids: endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin-3 (ET-3). All three isoforms are encoded by a 38-amino-acid precursor known as big endothelin. Endothelins are expressed in many tissues, including lung, kidney, brain, pituitary, and placenta. ...
To the best of our knowledge, this is the first study to demonstrate differences between aortic and coronary sinus endothelin concentrations in IDCM and to link ET-1 and BET plasma concentrations to the coronary circulation in regard to myocardial oxygen demand, coronary sinus oxygen content, and coronary blood flow at basal conditions in patients with IDCM.. As stated by other investigators,4 7 8 we found that in patients with IDCM with increasing NYHA class the plasma concentrations of immunoreactive ET-1/BET in arterial samples were increased. This was correlated with an increase in internal left ventricular dimensions and a decreased ejection fraction. An increment of ET-1/BET concentrations in venous samples of patients with CHF was described by Pacheret al and Pousset et al to be of prognostic importance, independent from haemodynamic data in patients with CHF.7 8 Therefore, our results are in accordance with the hypothesis that, with progressive heart failure, the endothelin system is ...
Endothelin receptor antagonists are approved for pulmonary arterial hypertension. Development of selective ETA-receptor antagonists over mixed or dual receptor antagonists has depended on a range of receptor binding assays, second messenger assays and functional blood vessel assays. This study compared the 3 clinically-approved endothelin receptor antagonists in assays of human isolated pulmonary and radial arteries in vitro. METHODS: Human isolated pulmonary (i.d. 5.5mm) and human radial (i.d. 3.23mm) artery ring segments were mounted in organ baths for isometric force measurement. Single concentration-contraction curves to endothelin-1 were constructed in the absence or presence of bosentan (1-10µM), macitentan (0.03-0.3µM) or ambrisentan (0.1-1µM). RESULTS: All 3 endothelin antagonists caused competitive rightward shifts in the endothelin-1 concentration-response curves in both arteries. The Clark plot and analysis gave the following pKB values: bosentan, pulmonary artery 6.28±0.13 and ...
TY - JOUR. T1 - Expression of a recombinant preproendothelin-1 gene in arteries stimulates vascular contractility. AU - Schott, Eckart. AU - Tostes, Rita C A. AU - San, Hong. AU - Paul, Martin. AU - Clinton Webb, R.. AU - Nabel, Elizabeth G.. PY - 1997/5/17. Y1 - 1997/5/17. N2 - Endothelin (ET)-l is a potent vasoconstrictor peptide that is elevated in cardiovascular diseases. However, the biological function of ET-1 gene expression within arteries in vivo has not been determined. The effects of ET-1 gene expression were investigated using gene-transfer methods on porcine vascular cells in vitro and porcine arteries in vivo. Transfection of vascular cells with a vector encoding for human preproendothelin-1 cDNA1 (pVR-ppET) resulted in significant increases in active ET-1 levels in culture supernatant compared with nontransfected cells (P , 0.05). This supernatant contracted rat aortic strips at concentrations 10-fold lower than synthetic ET-1 protein,. which was inhibited by the ET-A receptor ...
Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21) 142569-99-1 safety info, Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21) chemical safety search, Chemical Succinyl-(glu(9),ala(11,15))-endothelin-1 (8-21) safety technical specifications ect.
TY - GEN. T1 - Endothelin-1 potentiates cholinergic neurotransmission in rat trachea via ETA and ETB receptors. AU - Knott, P.G.. AU - Henry, Peter. AU - Goldie, Roy. PY - 1995. Y1 - 1995. M3 - Conference paper. VL - 2. SP - 99. BT - 29th Annual Scientific Meeting of the Australasian Society of Clinical and Experimental Pharmacologists and Toxicologist. PB - Australasian Society of Clinical and Experimental Pharmacologists and Toxicologists. CY - Sydney Australia. T2 - Endothelin-1 potentiates cholinergic neurotransmission in rat trachea via ETA and ETB receptors. Y2 - 1 January 1995. ER - ...
TY - JOUR. T1 - CD10 expressed by fibroblasts and melanoma cells degrades endothelin-1 secreted by human keratinocytes. AU - Xie, Lining. AU - Moroi, Yoichi. AU - Takahara, Masakazu. AU - Tsuji, Gaku. AU - Oba, Junna. AU - Hayashida, Sayaka. AU - Takeuchi, Satoshi. AU - Shan, Baoen. AU - Hiroshi, Uchi. AU - Furue, Masutaka. PY - 2011/9/26. Y1 - 2011/9/26. N2 - Endothelin-1 (ET-1) is a potent multifunctional peptide linked to wound healing, pigmentation, carcinogenesis, and fibrosclerotic processes in the skin. Whereas ET-1 was thought to be digested by receptor-mediated endocytosis, it is also reported to be biochemically degraded by the neutral endopeptidase CD10 using kidney homogenates. Although keratinocytes (KC) and fibroblasts (Fb) are sources of both ET-1 and CD10, respectively, there is no report investigating the direct association betweenCD10expression and its function in relation toET-1 degradation in the skin. CD10 expression in melanoma cells is associated with clinical prognosis, ...
TY - JOUR. T1 - Triglycerides impair postischemic recovery in isolated hearts. T2 - Roles of endothelin-1 and trimetazidine. AU - Monti, Lucilla D.. AU - Allibardi, Sonia. AU - Piatti, Pier Marco. AU - Valsecchi, Gianpietro. AU - Costa, Sabrina. AU - Pozza, Guido. AU - Chierchia, Sergio. AU - Samaja, Michele. PY - 2001. Y1 - 2001. N2 - There is growing evidence that hypertriglyceridemia exacerbates ischemic injury. We tested the hypothesis that triglycerides impair myocardial recovery from low-flow ischemia in an ex vivo model and that such an effect is related to endothelin-1. Hyperglycemic (glucose concentration = 12 mmol/l) and hyperinsulinemic (insulin concentration = 1.2 μmol/l) isolated rat hearts were perfused with Krebs-Henseleit buffer (PO 2 = 670 mmHg, pH 7.4, 37°C) added with increasing triglycerides (0, 1,000, 2,000, and 4,000 mg/dl, n = 6-9 rats/group). Hearts were exposed to 60 min of low-flow ischemia (10% of basal coronary flow), followed by 30 min of reperfusion. We found that ...
The purpose of this study was to investigate the effect of acute high intensity aerobic training on ANP and Endothelin-1 in inactive obese women. In order to nineteen obese women mean age± SD: 27.94± 3.30, mean weight ±SD: 88.13 ±7.28, mean height ±SD: 163.00± 4.91, mean BMI ±SD: 32.96± 3.13 selected and were randomly allocated to experimental and control groups. Experimental group performed a session acute aerobic exercise on ergometer at intensity 25w that increased every two minute 25w to workload and performed to exhaustion every subject. Samples blood were taken after 12 hours fasting, before and after of program training. For analyzed of biochemical variables used ELISA method and for analyses data used ANOVA. Results of this study showed that acute aerobic training causes significant increase in level of plasma ANP in obese women (p=0.006). But no significant differences observe in plasma level of Endothelin-1. Also, any significant difference didnt observe between pre and ...
in Equine Veterinary Journal (2003), 35(2), 190-6. Reasons for performing study: There is currently little published information about the effects of endothelin-1 (ET-1), a potent endogenous spasmogen of vascular and airway smooth muscle, on pulmonary ... [more ▼]. Reasons for performing study: There is currently little published information about the effects of endothelin-1 (ET-1), a potent endogenous spasmogen of vascular and airway smooth muscle, on pulmonary vasculature and airways or which ET receptor subtypes mediate ET-1 induced vasoconstrictive and bronchoconstrictive action in the horse. Objectives: To investigate the effect of endothelin-1 (ET-1) on smooth muscle from isolated equine pulmonary artery and bronchus. In addition, the roles of ETA and ETB receptors in ET-1 mediated contraction in these tissues were assessed. Methods: The force generation of ring segments from pulmonary arteries or third-generation airways (obtained from horses subjected to euthanasia for orthopaedic ...
INTRODUCTION: The aim of our study was to analyse the role of adrenomedullin (AM) and endothelin-1 (ET-1) in the adaptation of the maternal vascular system in normotensive pregnancy. METHODS: Twenty-eight pregnant women, who were normotensive through
TY - JOUR. T1 - The role of endothelin-1 during ischemia-reperfusion injury. AU - Chang, H.. AU - Wu, G. J.. AU - Wang, S. M.. AU - Hung, C. R.. PY - 1992. Y1 - 1992. UR - http://www.scopus.com/inward/record.url?scp=0027075162&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0027075162&partnerID=8YFLogxK. M3 - Article. C2 - 1363641. AN - SCOPUS:0027075162. VL - 91. SP - 1182. EP - 1188. JO - Journal of the Formosan Medical Association. JF - Journal of the Formosan Medical Association. SN - 0929-6646. IS - 12. ER - ...
TY - JOUR. T1 - Endothelin-1 in bronchoalveolar lavage during rejection of allotransplanted lungs. AU - Schersten, Henrik. AU - Aarnio, Pertti. AU - Burnett, John C.. AU - McGregor, Christopher G.A.. AU - Miller, Virginia M.. PY - 1994/1. Y1 - 1994/1. UR - http://www.scopus.com/inward/record.url?scp=0028107330&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=0028107330&partnerID=8YFLogxK. U2 - 10.1097/00007890-199401000-00027. DO - 10.1097/00007890-199401000-00027. M3 - Article. C2 - 8291104. AN - SCOPUS:0028107330. VL - 57. SP - 159. EP - 161. JO - Transplantation. JF - Transplantation. SN - 0041-1337. IS - 1. ER - ...
Sigma-Aldrich offers Sigma-E6139, Big Endothelin 2 human for your research needs. Find product specific information including CAS, MSDS, protocols and references.
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The protein encoded by this gene is a member of the endothelin family. Endothelins are endothelium-derived vasoactive peptides involved in a variety…
Correspondence to Dr. Masakazu Haneda, The Third Department of Medicine, Shiga University of Medical Science, Seta, Otsu, Shiga, 520-2192, Japan. Phone: 81-77-548-2222; Fax: 81-77-543-3858; E-mail: haneda{at}belle.shiga-med.ac.jp ...
Uppsala University, Medicinska vetenskapsområdet, Faculty of Medicine, Department of Genetics and Pathology. (Endocrine Pathology) ...
R. Wang, ,, Fischer, K., W Dashwood, M., Greenwood, J. A., Ho, E., Williams, D. E., Ashktorab, H., Dashwood, M. R., and Dashwood, R. H., Epigenetic inactivation of endothelin-2 and endothelin-3 in colon cancer., International journal of cancer. Journal international du cancer, vol. 132, no. 5, pp. 1004-12, 2013. ...
Endothelin-1 (ET-1) has been demonstrated to play a role in many physiological processes including vasoconstriction, cardiovascular homeostasis, inflammation, angiogenesis, and tissue regeneration. A critical step in the ...
The potent vasoconstrictor endothelin-1 (ET-1) is at its highest concentration in the normal human ejaculate and is associated with the progression of metastatic prostate cancer. ET-1 protein expression is detected in situ in 14 of 14 primary cancers and 14 of 16 metastatic sites of human prostatic carcinoma. Exogenous ET-1 induces prostate cancer proliferation directly and enhances the mitogenic effects of insulin-like growth factor I, insulin-like growth factor II, platelet-derived growth factor, basic fibroblast growth factor, and epidermal growth factor in serum-free conditions in vitro. The ETA-selective receptor antagonist A-127722 inhibits ET-1-stimulated growth, but the ETB-selective receptor antagonist BQ-788 does not. ET-3, an ETB-selective agonist, also had no effect on prostate cancer growth. No specific ETB-binding sites could be demonstrated in any established human prostate cancer cell line tested, and ETB mRNA, detected by reverse transcription PCR, was reduced. The predominance ...
TY - JOUR. T1 - Renal vasoconstriction to endothelin-1 is enhanced with blockade of endothelin-B receptors or nitric oxide production. AU - Stacy, D. L.. AU - Martinez, R.. AU - Tilton, Ronald. PY - 1996. Y1 - 1996. N2 - Endothelin (ET-1) is a potent renal vasoconstrictor causing an initial transient vasodilation due to activation of ETB receptors and a long-lasting vasoconstriction thought to be due to ETA and ETB receptors. In anesthetized rats ET-1 was infused intravenously {i.V., 1 nmole/kg) after BQ-123 (an ETA receptor antagonist), BQ-788 (an ETB receptor antagonist), or vehicle. Left renal artery flow and mean arterial pressure (MAP) were measured. Resistance was calculated as MAP/flow. ET-1 increased renal resistance by 248% (26±2 to 90±13 mmHg/ml/min.). After pretreatment with BQ-123 (1 mg/kg, i.V.), the increase in renal resistance with ET-1 was reduced by 77% (29±5 to 43±7 mmHg/ml/min.), due to a reduction in the increase in MAP by 81% and decrease in flow by 61%. Pretreatment ...
To determine the prognostic role of big endothelin-1 (ET-1) in left ventricular non-compaction cardiomyopathy (LVNC).We prospectively enrolled patients whose LVNC was diagnosed by cardiac MRI and who had big ET-1 data available. Primary end point was a composite of all-cause mortality, heart transplantation, sustained ventricular tachycardia/fibrillation and implanted cardioverter defibrillator discharge. Secondary end point was cardiac death or heart transplantation.Altogether, 203 patients (median age 44 years; 70.9% male) were divided into high-level (≥0.42 pmol/L) and low-level (,0.42 pmol/L) big ET-1 groups according to the median value of plasma big ET-1 levels. Ln big ET-1 was positively associated with Ln N-terminal pro-brain natriuretic peptide, left ventricular diameter, but negatively related to age and Ln left ventricular ejection fraction. Median follow-up was 1.9 years (IQR 0.9-3.1 years). Kaplan-Meier analysis showed that, compared with patients with low levels of big ET-1, ...
Fingerprint Dive into the research topics of The endothelin-converting enzyme-1/endothelin-1 pathway plays a critical role in inflammation-associated premature delivery in a mouse model. Together they form a unique fingerprint. ...
TY - JOUR. T1 - Heparin regulates endothelin production through endothelium-derived nitric oxide in human endothelial cells. AU - Yokokawa, Koji. AU - Tahara, Hideki. AU - Kohno, Masakazu. AU - Mandal, Anil K.. AU - Yanagisawa, Masashi. AU - Takeda, Tadanao. PY - 1993. Y1 - 1993. N2 - Heparin shows blood pressure lowering effect in hypertensive patients and animal models. The present study examined the effect of heparin on vasoconstrictor endothelin-1 (ET-1) production in cultured human umbilical vein endothelial cells (ECs) to elucidate the mechanism of antihypertensive effect of heparin. Heparin suppressed both basal and thrombin-stimulated ET-1 mRNA expression paralleled with a decrease in ET-1 peptide release in a dose-dependent manner. Heparin concomitantly enhanced nitric oxide (NO) formation measured by NO2/NO3 levels and cGMP production in ECs. These enhancements were more marked when ECs were stimulated by thrombin. However, these heparins effects were blunted in the presence of ...
Endothelin-1, angiotensin II, and oxygen-derived radicals are pivotal factors in the development and progression of atherosclerosis. In vitro studies suggest that generation of oxygen-derived radicals by angiotensin II is an important mechanism increasing endothelin-1 synthesis, which consecutively may trigger effects such as cell proliferation and hypertrophy. The aim of this study was to confirm our previous data in an ex vivo and an in vivo setting.. Explanted segments of internal mammary arteries were analyzed for big endothelin-1 expression following incubation with xanthine oxidase, angiotensin II, superoxide dismutase, and catalase to stimulate or to specifically inactivate oxygen-derived radicals. Endothelin-1 concentrations were determined by immunostaining and enzyme-linked immunosorbent assay. Further, oxypurinol was given to patients undergoing coronary angioplasty, a procedure known to increase plasma endothelin-1 concentrations.. Angiotensin II and xanthine oxidase dose-dependently ...
ET (endothelin)-1, a potent vasoconstrictor peptide released by the endothelium, plays an important role in vasomotor regulation and has been linked to diminished endothelial vasodilator capacity in several pathologies associated with human aging, including hypertension, Type 2 diabetes and coronary artery disease. However, it is currently unknown whether the decline in endothelial vasodilatation with advancing age is due to elevated ET-1 vasconstrictor activity. Accordingly, we tested the hypothesis that the age-related impairment in ACh (acetylcholine)-mediated endothelium-dependent vasodilatation is due, at least in part, to increased ET-1-mediated vasoconstrictor tone. FBF (forearm blood flow) responses to ACh, SNP (sodium nitroprusside) and BQ-123 (ETA receptor blocker) were determined in 14 young (age, 25±1 years) and 14 older (age, 61±2 years) healthy non-obese men. Additionally, FBF responses to ACh were determined in the presence of ETA blockade. Vasodilatation to ACh was lower ...
The BP-lowering effects of nebivolol are well established.13,27,28 The seminal and novel finding of the present study, however, is that in addition to, and independent of, lowering BP, nebivolol markedly and favorably affects ET-1 system activity. Indeed, the results reported herein demonstrate that (1) chronic nebivolol, but not metoprolol, therapy reduces ET-1-mediated vasoconstrictor tone in adults with elevated BP and (2) reductions in ET-1 vasoconstriction underlie nebivolol-induced improvements in endothelium-dependent vasodilation. Diminished ET-1-mediated vasoconstrictor tone may represent an important endovascular pleiotropic effect of nebivolol, contributing to its favorable effect on overall cardiovascular risk.29. In this study, there was a similar and significant (≈30%) increase in FBF responses to selective ETA receptor blockade in all 3 groups before treatment. In addition, nonselective ETA/B receptor blockade resulted in a further increase (≈35%) in FBF in all the groups. ...
TY - JOUR. T1 - Central obesity and hypertension: the role of plasma endothelin. Am J Hypertens. AU - Licata, Giuseppe. AU - Corrao, Salvatore. AU - Scaglione, Rosario. AU - Parrinello, Gaspare. AU - Licata, Anna. AU - Pinto, Antonio. AU - Parrinello, Gaspare. PY - 1996. Y1 - 1996. N2 - Hypertension and central obesity are two conditions closely linked, but the mechanisms responsible for obesity-associated hypertension are still unclear. In the last few years, several studies addressed the role of endothelin-1 (ET-1) in the development and maintenance of hypertension. This study was designed to evaluate plasma ET-1 in normotensive and hypertensive central obese subjects compared with a lean healthy group. Our final goal was to analyze the relationship between plasma ET-1, blood pressure, and left ventricular structure and function in central obese subjects (both normotensives and hypertensives). ET-levels have been assessed by the radioimmunoassay method in 20 lean normotensives and in 57 ...
Using Na+/Ca2+ exchanger (NCX1)-deficient mice, the pathophysiological role of Ca2+ overload via the reverse mode of the Na+/Ca2+ exchanger in ischaemia/reperfusion-induced renal injury was investigated. Since NCX1-/- homozygous mice die of heart failure before birth, we utilized NCX1+/- heterozygous mice. The ischaemia/reperfusion-induced renal dysfunction in heterozygous mice were significantly attenuated compared with cases in wild-type mice. Also, histological renal damage such as tubular necrosis and proteinaceous casts in tubuli in heterozygous mice were much less than that in wild-type mice. Ca2+ deposition in necrotic tubular epithelium was observed more markedly in wild-type than in heterozygous mice. The increase in renal endothelin-1 (ET-1) content was significantly greater in wild-type than in heterozygous mice, and this reflected the difference in immunohistochemical ET-1 localization in necrotic tubular epithelium. We conclude that Ca2+ overload via the reverse-mode of Na+/Ca2+ ...
TY - JOUR. T1 - Endothelin-1 increases expression of cyclooxygenase-2 and production of interlukin-8 in hunan pulmonary epithelial cells. AU - Peng, Hong. AU - Chen, Ping. AU - Cai, Ying. AU - Chen, Yan. AU - Wu, Qing hua. AU - Li, Yun. AU - Zhou, Rui. AU - Fang, Xiang. PY - 2008/3. Y1 - 2008/3. N2 - Inducible cyclooxygenase (COX-2) and inflammatory cytokines play important roles in inflammatory processes of chronic obstructive pulmonary disease (COPD). Endothelin-1 (ET-1) might be also involved in the pathophysilogical processes in COPD. In the present study, we determined whether ET-1 could regulate the expression of COX-2 and alter the production of interleukin-8 (IL-8) in human pulmonary epithelial cells (A549). Induced sputum samples were collected from 13 stable COPD patients and 14 healthy subjects. The COX-2 protein, ET-1, PGE2 and IL-8 in these sputum samples were analyzed. A549 cells were incubated with ET-1 in the presence or absence of celecoxib, a selective COX-2 inhibitor. The ...
Endothelial cells were isolated from bovine thoracic aorta and cultured. Bovine aortic endothelial cells (BAEC) were incubated with radiolabeled arachidonic acid (3H-AA) or eicosapentaenoic acid (14C-EPA) (1 microM) for 3 hr. Both fatty acids were predominantly incorporated into phosphatidylcholine (57 +/- 2% and 62 +/- 2% respectively) and slightly into phosphatidylethanolamine (11 +/- 0.5% and 12 +/- 0.6% respectively). phosphatidylinositol (26 +/- 1.5% and 10 +/- 0.5% respectively) and neutral lipids (6 +/- 0.5% and 15 +/- 1% respectively). After BAEC incubation with 3H-AA for 24 hr with or without EPA (1 microM), the release of radioactive metabolites of AA induced by thrombin (5.5 U/ml) was strongly reduced by the preliminary treatment with EPA (72 +/- 5%). After BAEC incubation with AA, EPA or vehicle (control), endothelin-1 levels were measured by RIA in the culture medium and we observed that: 1) the basal production of endothelin-1 was not modified after either AA or EPA treatment, 2) the
Various tissues including heart express specific binding sites for endothelin. Endothelins have been reported to increase the force of contraction of cardiac muscle, presumably via specific receptors. Specific binding of endothelin to atrial tissue is particularly high. In spontaneously contracting rat atrial cells used in this study, all three isoforms of endothelin (endothelin-1, endothelin-2, and endothelin-3) decreased the rate of beating and caused an increase in inwardly rectifying K+ current in voltage-clamped whole cells. Endothelin-3 was the most potent isoform, and its effects on beating rate and K+ current were present at a concentration as low as 100 pM (Kd, approximately 1 nM). the atrial cells did not have the hyperpolarization-activated current (the pacemaker current), If. In excised inside-out patches, all three isoforms of endothelin activated a population of K+ channels with kinetic properties identical to those of acetylcholine (muscarinic)-activated K+ channels, and this was ...
Endothelin is the most potent constrictor of human blood vessels known to man. In mammals, there are three structurally and pharmacologically separate ET isopeptides: ET-1, ET-2, and ET-3 (Volpe 46). Endothelin-1 is the primary isoform in the human cardiovascular system and is a 21-amino acid peptide produced chiefly by endothelial cells (Lüscher 2434). Endothelin-converting enzymes (ECE), chymases, and non-ECE metalloproteases are responsible for the synthesis of ET-1 by means of autocrine regulation (Lüscher 2434). ET-1 operates through the initiation of two G-protein coupled receptors: ETA and ETB. Located on vascular smooth muscle cells, ETA receptors regulate vasoconstriction and cell proliferation. ETB receptors, situated on endothelial cells, mediate endothelium-dependent vasodilation through the release of nitric oxide and prostacyclin (Haapaniemi 721). In addition to its cardiovascular and mitogenic effects, endothelin-1 is involved in gastrointestinal and endocrine function, ...
The major findings of this study are that ET-1 prevents apoptosis induced by serum deprivation in a dose-dependent manner via an ETA receptor in H9c2 cardiomyocytes and that the antiapoptotic effect of ET-1 is mediated through a c-Src/Bcl-xL pathway. Evidence for this proposal includes the following: (1) ET-1, but not AII, prevented mitochondrial cytochrome c release and apoptosis induced by serum deprivation in a dose-dependent manner, and this antiapoptotic effect was inhibited by an ETA receptor antagonist (BQ123) but not by an ETB receptor antagonist (BQ788); (2) the inhibitory effects of ET-1 on apoptosis were inhibited by tyrosine kinase inhibitors and adenovirus-mediated overexpression of KI-c-Src; (3) ET-1 stimulated c-Src activation; and (4) ET-1 upregulated an antiapoptotic molecule, Bcl-xL, and this upregulation was inhibited by tyrosine kinase inhibitors or cotransfection with KI-c-Src.. Recent evidence suggests that apoptosis of cardiac myocytes is a feature in cardiovascular ...
The mitogenic activity of endothelin and its ability to stimulate PtdIns(4,5)P2 and phosphatidylcholine turnover in Rat-1 fibroblasts was studied. Stimulated incorporation of [3H]thymidine occurred in the absence of any other added growth factors. The endothelins stimulated rapid generation of both Ins(1,4,5)P3 and choline. Endothelin-1 and endothelin-2 were equipotent in stimulating both responses, but endothelin-3 was less potent. Endothelin-1-stimulated Ins(1,4,5)P3 generation reached a maximum at 5 s and then declined; however, the response was long-lived, with a 4.5-fold elevation over basal still observed after 15 min. Endothelin-stimulated choline generation was observed with no increase in choline phosphate; indeed, the apparent level of this metabolite fell after 30 min of stimulation, presumably due to the observed stimulation of phosphatidylcholine synthesis. The endothelin-stimulated increase in choline generation was abolished in cells where protein kinase C was down-regulated. ...
Concentrations of angiotensin II, endothelin-1, and BNP in the coronary sinus and ascending aorta of patients with heart disease ...
Pathology: 1997-1998. ARMSTRONG, R.. Atkison, P.R., G.I. Joubert, C.M. Guiraudon, R. Armstrong, W. Wall, S. Asfar, and D. Grant. 1997. Arteritis and increased intracellular calcium as a possible mechanism for tacrolimus-related cardiac toxicity in a pediatric transplant recipient. Transplantation 64 (5): 773-775.. CHAKRABARTI, S.. Adams, P.C., and S. Chakrabarti. 1998. Genotypic/phenotypic correlations in genetic hemochromatosis: evolution of diagnostic criteria. Gastroenterology 114 (2): 319-323.. Chakrabarti, S., X.T. Gan, A. Merry, M. Karmazyn, and A.A.F. Sima. 1998. Augmented retinal endothelin-1, endothelin-3, endothelinA and endothelinB gene expression in chronic diabetes. Current Eye Research 17: 301-307.. Chakrabarti, S., and A.A.F. Sima. 1997. Endothelin-1 and endothelin-3-like immunoreactivity in the eyes of diabetic and non-diabetic bb/w rats. Diabetes Research and Clinical Practice 37: 109-120.. Deng, D.X., S. Chakrabarti, M.P. Waalkes, and M.G. Cherian . 1998. Metallothionein and ...
Dive into the research topics of EFFECT OF POST-ISCHEMIC MILD HYPOTHERMIA ON THE LEVELS OF IMPORTANT CYTOKINES IN THE ENDOTHELIN-1 RAT MODEL FOR FOCAL CEREBRAL ISCHEMIA. Together they form a unique fingerprint. ...
back to overview Endothelins are vasoconstricting peptides produced by vascular endothelial cells. The endothelin family consists of three members, endothelin-1; endothelin-2; and endothelin-3.. back to overview ...
Endothelin A Receptor: A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
This gene encodes a member of the endothelin protein family of secretory vasoconstrictive peptides. The preproprotein is processed to a short mature form which functions as a ligand for the endothelin receptors that initiate intracellular signaling events. This gene product is involved in a wide range of biological processes, such as hypertension and ovulation. Altered expression of this gene is implicated in tumorigenesis. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Oct 2014 ...
Multiple myeloma (MM) can be an indolent B-cell disease that develops in the bone tissue marrow and it is connected with osteolytic lesions in 1174043-16-3 the advanced phases [1]. site thats turned on in Tyr1356 and Tyr1349. The phosphorylation of the region leads to the induction of MET signaling through the activation of many downstream …Read More. ...
Background: Endothelin-1 and Endostar are both significant for the progression, proliferation, metastasisand invasion of cancer. In this paper, we studied the effect of ET-1 RNAi and Endostar in PC-3 prostatic cancercells. Materials and Methods: The lentiviral vector was used in the establishment of ET-1 knockdown PC-3 cells.Progression and apoptosis were assessed by CKK-8 and flow cytometry, respectively. Transwell assay was usedto estimate invasion and signaling pathways were studied by Western blotting. Results: ET-1 mRNA and proteinin ET-1 knockdown PC-3 cells were reduced to 26.4% and 22.4% compared with control group, respectively.ET-1 RNAi and Endostar both were effective for the suppression of progression and invasion of PC-3 cells.From Western blotting results, the effects of ET-1 regulation and Endostar on PC-3 cells were at least relatedto some signaling pathways involving PI3K/Akt/Caspase-3, Erk1/2/Bcl-2/Caspase-3 and MMPs (MMP-2 andMMP-9). Furthermore, combined treatment of ET-1RNAi and
Exposure to air pollution negatively impacts cardiovascular health. Studies show that increased exposure to a number of airborne pollutants increases the risk for cardiovascular disease progression, m
Ala(1,3,11,15)- endothelin 1: alanyl residues substituted for cysteinyl in endothelin-1; RN given refers to (all-L)-isomer; has been used as a radioligand, highly selective for ET(B) receptor
Endothelin-1 is a potent vasoconstrictor in the body. Previous studies have identified associations between the coding polymorphism K198N and hypertension, systolic blood pressure and HDL levels. We s
Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Rev. Invest. Clin. 59 (1): 48- ... 211 (1): 234-40. doi:10.1006/bbrc.1995.1801. PMID 7779090. Ma JX, Wang DZ, Ward DC, et al. (1995). "Structure and chromosomal ... 184 (1): 260-8. doi:10.1016/0006-291X(92)91187-U. PMID 1314587. Eggerickx D, Raspe E, Bertrand D, et al. (1992). "Molecular ... 211 (1): 226-33. doi:10.1006/bbrc.1995.1800. PMID 7779089. Braun A, Kammerer S, Böhme E, et al. (1995). "Identification of ...
"Increased pulmonary vascular endothelin B receptor expression and responsiveness to endothelin-1 in cirrhotic and portal ... Endothelin-1 has two receptors in the pulmonary arterial tree, ET-A which mediates vasoconstriction and ET-B which mediates ... Gerbes, AL; Møller, S; Gülberg, V; Henriksen, JH (March 1995). "Endothelin-1 and -3 plasma concentrations in patients with ... Giaid, A (September 1998). "Nitric oxide and endothelin-1 in pulmonary hypertension". Chest. 114 (3 Suppl): 208S-212S. doi: ...
Endothelin is a potent vasoactive peptide produced by endothelial cells that has both vasoconstrictor and vasodilator ... Circulating endothelin levels are increased in some hypertensive patients, particularly African Americans and persons with ... For example, local nitric oxide and endothelin, which are secreted by the endothelium, are the major regulators of vascular ... Ergul S, Parish DC, Puett D, Ergul A (October 1996). "Racial differences in plasma endothelin-1 concentrations in individuals ...
Endothelin-converting enzyme-like 1 is a protein that in humans is encoded by the ECEL1 gene. This gene encodes a member of the ... "Entrez Gene: ECEL1 endothelin converting enzyme-like 1". Valdenaire O, Rohrbacher E, Langeveld A, et al. (2000). "Organization ... Valdenaire O, Richards JG, Faull RL, Schweizer A (Mar 1999). "XCE, a new member of the endothelin-converting enzyme and neutral ... Benoit A, Vargas MA, Desgroseillers L, Boileau G (2004). "Endothelin-converting enzyme-like 1 (ECEL1) is present both in the ...
Mawji IA, Marsden PA (June 2006). "RNA transfection is a versatile tool to investigate endothelin-1 posttranscriptional ... Endothelin-1) with potential applications in gene therapy. Limitation of the silencing approach are the toxicity of the ... 38 (1): 48-52. doi:10.2144/05381bm05. PMID 15679084. Jacobsen LB, Calvin SA, Colvin KE, Wright M (June 2004). "FuGENE 6 ... 20 (1): 81-9. doi:10.1111/j.1472-8206.2005.00344.x. PMID 16448398. S2CID 42585711. Sapra, Rachit; Verma, Ram P.; Maurya, Govind ...
These endothelial products include nitric oxide and endothelin-1 that are released in response to either chemical stimuli, like ... endothelin-1 causes vasoconstriction. Below are several examples of differing types of local blood flow regulation by specific ... ISBN 978-1-60913-241-5. OCLC 781683439. "Tubuloglomerular Feedback". www.pathwaymedicine.org. Retrieved 2019-12-18. "Pulmonary ...
This binding initiates the same intracellular signalling pathways as angiotensin and endothelin. There is also activation of ... Angiotensin-II and endothelin-1 are hormones that bind to the angiotensin (AT) and endothelin (ET) receptors. These are G- ... endothelin-1 and the catecholamines (e.g. noradrenaline).[citation needed] ... 92 (Supp 1): i2-i13. doi:10.1136/hrt.2005.077875. PMC 1860731. PMID 16543598. van der Bruggen, C (2017). "RV pressure overload ...
"Mast cells promote homeostasis by limiting endothelin-1-induced toxicity". Nature. 432 (7016): 512-6. doi:10.1038/nature03085. ... 89 (1): 273-82. doi:10.1172/JCI115571. PMC 442845. PMID 1729276. Huang H, Reed CP, Zhang JS, Shridhar V, Wang L, Smith DI (June ... 184 (1): 99-105. doi:10.1016/0022-2836(85)90046-4. PMID 4032478. Kokkonen JO, Vartiainen M, Kovanen PT (December 1986). "Low ... is also reported to have an important role in the protection towards snake venom toxins and vasoconstricting peptide endothelin ...
4-Diarylpyrrolidine-3-carboxylic AcidsPotent ETASelective Endothelin Receptor Antagonists. 1. Discovery of A-127722". Journal ... 6 (1): 12-22. Yamada, Shun-Ichi; Fujii, Tozo; Shioiri, Takayuki (1962). "Studies on Optically Active Amino Acids. I. ... Piperonal can be prepared by the oxidative cleavage of isosafrole or by using a multistep sequence from catechol or 1,2- ...
7003106022800000000♠1060.228 g·mol−1 Except where otherwise noted, data are given for materials in their standard state (at 25 ... The B1 receptor (also called bradykinin receptor B1) is expressed only as a result of tissue injury, and is presumed to play a ... This receptor has been also described to play a role in inflammation.[10] Most recently, it has been shown that the kinin B1 ... The kinin B1 and B2 receptors belong to G protein coupled receptor (GPCR) family. ...
Plates containing puromycin are stable for 1 month when stored at 4 [7]°C.[citation needed] ... Puromycin is an aminonucleoside antibiotic, derived from the Streptomyces alboniger bacterium,[1] that causes premature chain ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... The recommended dose as a selection agent in cell cultures is within a range of 1-10 μg/ml, although it can be toxic to ...
1 (6): 588-90. doi:10.1097/01243894-200607000-00016. PMID 17409923.. *^ He J, Zhang A, Fang M, Fang R, Ge J, Jiang Y, Zhang H, ... Binding proteins: IGFBP (1, 2, 3, 4, 5, 6, 7). *Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1) ... IGF-2 exerts its effects by binding to the IGF-1 receptor and to the short isoform of the insulin receptor (IR-A or exon 11-).[ ... doi:10.1016/S0074-7696(05)43004-1. ISBN 9780123646477. . PMID 15797461.. *. Fowden AL, Sibley C, Reik W, Constancia M (2006). " ...
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... 2S)-2-[[(3aS,7aS)-1-[2-[(2S)-2-[[(2S)-. 2-[[2-[[(4R)-1-[1-[2-[[(2R)-2-amino-5-(diaminomethylideneamino). pentanoyl]amino]-5-( ... Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Sarafotoxin. *Antagonists: A-192621 ...
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... Intestinal GLP-2 is co-secreted along with GLP-1 upon nutrient ingestion. ... GLP-1). GLP-2 is produced by the intestinal endocrine L cell and by various neurons in the central nervous system. ... post-translational proteolytic cleavage of proglucagon in a process that also liberates the related glucagon-like peptide-1 ( ...
... reliably causes severe anxiety symptoms when administered to humans in a dose of as little as 50μg,[1] and is commonly ... 3S)-3-[(2S)-2-amino-3-phenylpropanamido]-3-{[(1S)-1-{[(1S)-1-carboxy -2-(indol-3-yl)ethyl]carbamoyl}-3-(methylsulfanyl)propyl] ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Sarafotoxin. *Antagonists: A-192621 ...
Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Antagonists: A-192621 ... N-[(3R,6S)-6-(2,3-Difluorophenyl)hexahydro-2-oxo-1-(2,2,2-trifluoroethyl)-1H-azepin-3-yl]-4-(2,3-dihydro-2-oxo-1H-imidazo[4,5-b ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ...
668 (1 The Neurobiol): 30-42. doi:10.1111/j.1749-6632.1992.tb27337.x. PMID 1463273.. ... 668 (1 The Neurobiol): 1-16. doi:10.1111/j.1749-6632.1992.tb27335.x. PMID 1463268.. .mw-parser-output cite.citation{font-style: ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... 1-6H3,(H,41,49)(H,42,50)(H,43,48)(H,44,47)(H,52,53)/t23-,24-,27-,28-,29-,30-,31-,32-/m0/s1 ...
Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Antagonists: A-192621 ... 8 (1): 216. doi:10.1186/1471-2105-8-216. PMC 1920535 . PMID 17587460.. CS1 maint: Multiple names: authors list (link) CS1 maint ... ISBN 978-1-58829-399-2. PMID 16350956.. *^ Marquet P, Lachâtre G; Lachâtre (October 1999). "Liquid chromatography-mass ... GHRH 1-24 (Growth Hormone Releasing Hormone 1-24) ... 1][2] Proteins consist of one or more polypeptides arranged in ...
Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Sarafotoxin. *Antagonists: A-192621 ...
978-1-4160-3661-6. .. *^ Cozzi, Bruno; Huggenberger, Stefan; Oelschläger, Helmut (2017-01-01). "Chapter 7 - Body Control: The ... The PPY gene encodes an unusually short protein precursor.[1] This precursor is cleaved to produce pancreatic polypeptide, ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... Washabau, Robert J. (2013). "Chapter 1 - Integration of Gastrointestinal Function". Canine and Feline Gastroenterology. ...
... (/ɒˈrɛksɪn/), also known as hypocretin, is a neuropeptide that regulates arousal, wakefulness, and appetite.[1] The most ... 25 (1): 173-83. doi:10.1523/JNEUROSCI.4015-04.2005. PMID 15634779.. *^ Yamanaka A, Muraki Y, Ichiki K, Tsujino N, Kilduff TS, ... The orexin peptides bind to the two G-protein coupled orexin receptors, OX1 and OX2, with orexin-A binding to both OX1 and OX2 ... 96 (1): 284-98. CiteSeerX 10.1.1.320.260. doi:10.1152/jn.01361.2005. PMID 16611835.. ...
298 (1): E99-E107. doi:10.1152/ajpendo.00242.2009. PMID 19843871.. *^ a b Pittner RA, Albrandt K, Beaumont K, Gaeta LS, Koda JE ... 257 (1): 179-85. doi:10.1007/BF00221649. PMID 2546670.. *. Nishi M, Sanke T, Seino S, et al. (1990). "Human islet amyloid ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... A non-fibril forming peptide (1-19 residues of human amylin) is toxic like the full-length peptide but the respective segment ...
978-1-4614-6198-2. . PMC 4019505. PMID 23550004.. *^ Arai AC (January 2009). "The role of kisspeptin and GPR54 in the ... "Entrez Gene: KISS1 KiSS-1 metastasis-suppressor".. *^ De Bond JA, Smith JT (March 2014). "Kisspeptin and energy balance in ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... Lee JH, Miele ME, Hicks DJ, Phillips KK, Trent JM, Weissman BE, Welch DR (December 1996). "KiSS-1, a novel human malignant ...
Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Antagonists: A-192621 ... 73 (1): 114-116. doi:10.1016/s0015-0282(99)00450-1.. *^ Williams, R. Stan; et al. (2003). "Pregnancy rates in varying age ... 1, 2011. *^ Dickey, RP; Thornton, M; Nichols, J; Marshall, DC; Fein, SH; Nardi, RV (Jun 2002). "Comparison of the efficacy and ... ISBN 1-904798-96-9. Page 44.. *^ Follicle Stimulating Hormone and Luteinizing Hormone (Intramuscular Route, Subcutaneous Route) ...
doi:10.1016/S1474-4422(14)70209-1. PMID 25297013. S2CID 206161999.. *^ "International Nonproprietary Names for Pharmaceutical ... 143283.20 g·mol−1. Eptinezumab, sold under the brand name Vyepti, is a medication for the preventive treatment of migraine in ... Trial 1 enrolled subjects with a history of episodic migraine headaches and Trial 2 enrolled subjects with chronic migraine ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ...
doi:10.1016/0076-6879(95)48016-1. ISBN 9780121821494. PMID 7674923.. *^ US 2130505, Münz, F., "Polyamino carboxylic acids", ... InChI=1S/C10H16N2O8/c13-7(14)3-11(4-8(15)16)1-2-12(5-9(17)18)6-10(19)20/h1-6H2,(H,13,14)(H,15,16)(H,17,18)(H,19,20) Y ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ... 1,2-diaminoethane), formaldehyde, and sodium cyanide.[19] This route yields the tetrasodium EDTA, which is converted in a ...
... , which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin ... As such, endothelin receptor antagonists such as Ambrisentan are known to be teratogenic. Ambrisentan has a high risk of liver ... Endothelin receptor activation mediates strong pulmonary vasoconstriction and positive inotropic effect on the heart. These ... In addition to this, endothelin receptors are also known to play a role in neural crest cell migration, growth, and ...
His publications include first-in-human studies with renin inhibitors and endothelin antagonists, including exploration of the ... Haynes WG, Webb DJ (September 1994). "Contribution of endogenous generation of endothelin-1 to basal vascular tone". Lancet. ... Dhaun N, Webb DJ (August 2019). "Endothelins in cardiovascular biology and therapeutics". Nature Reviews. Cardiology. 16 (8): ... role of endothelin antagonists as treatment for vascular and renal disease. He has also contributed to the current ...
She primarily tests rats and uses the Endothelin-1 stroke model. Her most recent work has expanded into the field of ... Theresa Jones was born in Pine Bluff, Arkansas on November 1, 1964. Throughout her childhood, her family moved around to Little ... CS1 maint: discouraged parameter (link) Jones, TA (1 April 1994). "Use-Dependent Growth Of Pyramidal Neurons After Neocortical ... 1): 156-160 May 22, 1992 Times Cited: 148 Jones TA, Chu Cj, Grande La, Et Al. "Motor Skills Training Enhances Lesion-Induced ...
... and thus activate endothelin-receptors, endothelin receptor type A (ETA) and endothelin receptor type B (ETB). These receptors ... Lüscher TF, Barton M (November 2000). "Endothelins and endothelin receptor antagonists: therapeutic considerations for a novel ... Together with endothelins (ETs), they form a homogenous family of strong vasoconstrictor isopeptides. Among them, few slightly ... The main differences in the family of endothelin and sarafotoxins appear at N-terminal of peptides, as C-terminal in all of ...
Endothelin receptor antagonist(英語:Endothelin receptor antagonist). *NK1 receptor antagonist(英語:NK1 receptor antagonist) ... 腎上腺素(Epinephrine或Adrenaline), 3,4-三羥基-N-甲基苯乙胺。是腎上腺髓質分泌的激素及神經傳導物質,也是一種藥物[3][4]。腎上腺素被應用於治療多項疾病,包含
Wang Y, Macke JP, Abella BS, Andreasson K, Worley P, Gilbert DJ, Copeland NG, Jenkins NA, Nathans J (Jun 1996). "A large family of putative transmembrane receptors homologous to the product of the Drosophila tissue polarity gene frizzled". J Biol Chem. 271 (8): 4468-76. doi:10.1074/jbc.271.8.4468. PMID 8626800 ...
1-59541-101-1. .. *^ a b Nichols AJ, Ruffolo RR, Brooks DP (June 1990). "The pharmacology of fenoldopam". Am. J. Hypertens. 3 ( ... Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... InChI=1S/C16H16ClNO3/c17-15-11-5-6-18-8-13(9-1-3-10(19)4-2-9)12(11)7-14(20)16(15)21/h1-4,7,13,18-21H,5-6,8H2 Y ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ...
11 (1): 90-4. doi:10.1038/nm1168. PMID 15619630.. *. Oh JH, Yang JO, Hahn Y, Kim MR, Byun SS, Jeon YJ, Kim JM, Song KS, Noh SM ... "Free fatty acids regulate gut incretin glucagon-like peptide-1 secretion through GPR120". Nat. Med. ...
InChI=1S/C26H32N4O4S/c1-20(2)30(16-10-11-17-34-19-24(31)29-35(3,32)33)23-18-27-25(21-12-6-4-7-13-21)26(28-23)22-14-8-5-9-15-22/h4-9,12-15,18,20H,10-11,16-17,19H2,1-3H3,(H,29,31) ...
Barnes K, Turner AJ (August 1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and cellular ... Agapitov AV, Haynes WG (March 2002). "Role of endothelin in cardiovascular disease". J Renin Angiotensin Aldosterone Syst 3 (1 ... Gross PM, Zochodne DW, Wainman DS, Ho LT, Espinosa FJ, Weaver DF (July 1992). "Intraventricular endothelin-1 uncouples the ... "The vascular endothelin system in hypertension--recent patents and discoveries". Recent Pat Cardiovasc Drug Discov 1 (1): 95- ...
107 (1): 89-91. doi:10.1007/s004390050017. PMID 10982042.. *. Otsuki T, Ota T, Nishikawa T, Hayashi K, Suzuki Y, Yamamoto J, ... "Physical mapping and exclusion of GPR34 as the causative gene for congenital stationary night blindness type 1". Human Genetics ...
Takagi, Y.; Fukase, M.; Takata, S.; Yoshimi, H.; Tokunaga, O.; Fujita, T. (1990-04-30) «Autocrine effect of endothelin on DNA ... Ingelesez) Lewontin, R C (1970-11) «The Units of Selection» Annual Review of Ecology and Systematics (1): 1-18 doi:10.1146/ ... ISBN 1-4051-1950-0 *↑ Radding, Charles M. (1982-12-01) «Homologous pairing and strand exchange in genetic recombination» Annual ... Lande, R (1989) «Fisherian and Wrightian theories of speciation» Genome 31 (1): 221-7 2687093 . Noiz kontsultatua: 2010-06-09. ...
This article on a gene on human chromosome 1 is a stub. You can help Wikipedia by expanding it.. *v ... Binding proteins: IGFBP (1, 2, 3, 4, 5, 6, 7). *Cleavage products/derivatives with unknown target: Glypromate (GPE, (1-3)IGF-1) ... 95 (1): 221-30. PMID 10607706.. *. Munthe E, Aasheim HC (2002). "Characterization of the human ephrin-A4 promoter". Biochem. J ... are clustered on human chromosome 1 and mouse chromosome 3". Genomics. 33 (2): 277-82. doi:10.1006/geno.1996.0192. PMID 8660976 ...
In the study and discussion of equine coat color genetics, black is considered a "base" color, as is red. This designation makes the effects of other coat color genes easier to understand. Coat colors that are designated "black-based" include grullo (also called blue dun), smoky black, smoky cream, silver black, classic champagne, and blue roan. Sometimes this designation includes the bay family: bay, seal brown, buckskin, bay dun, silver bay, perlino, amber champagne, and bay roan. Horses with a black-based coat may also have added spotting patterns including leopard patterns seen on Appaloosas and the pinto coloring known as piebald. The genetics behind the black horse are relatively simple. The color black is primarily controlled by two genes: Extension and Agouti. The functional, dominant allele of the extension gene (labeled "E") enables the horse to produce black pigment in the hair. Without this gene (homozygous recessive condition "ee"), the coat is devoid of black pigment and the horse ...
108 (1): 238-63. doi:10.1021/cr0682195. PMID 18181659.. *^ Cristalli G, Lambertucci C, Marucci G, Volpini R, Dal Ben D (2008 ... A1 adenosine receptor[edit]. Main article: Adenosine A1 receptor. The adenosine A1 receptor has been found to be ubiquitous ... Tecadenoson is an effective A1 adenosine agonist, as is selodenoson. In the heart[edit]. The A1, together with A2A receptors of ... The adenosine receptors (or P1 receptors[1]) are a class of purinergic G protein-coupled receptors with adenosine as the ...
It can inhibit endothelin converting enzymes even in the live rat, probably by chelating metals required by metalloproteases. ... Huggins, John P.; Pelton, John T. (1996-12-23). Endothelins in Biology and Medicine. CRC Press. p. 121. ISBN 9780849369759. ... "Pharmacological profiles of aspergillomarasmines as endothelin converting enzyme inhibitors". The Japanese Journal of ... Anhydroaspergillomarasmine A, a lactam of aspergillomarasmine A, chemically called [1-(2-amino-2carboxyethyl)-6-carboxy-3- ...
... and endothelin receptor antagonists have no effect, and in some cases worsen of the EIPH. ... Epistaxis (blood coming from one or both nostrils) is much less common, occurring in 0.25-13% of cases.[1][9] In a survey of ... 978-0-9654461-1-2. .. *Roberts, C.A., Hillidge, C. and Marlin, D.J. (1993) Exercise induced pulmonary haemorrhage in racing ... EIPH also occurs in eventers, jumpers, polo ponies, endurance horses, draft horses that pull competitively,[1] and horses ...
However, one form for which there is a DNA test, the sabino-1 (SB1) gene, is a dominant. Horses homozygous for SB-1 sometimes ... Sabino-1 and other sabino patterns are not associated with any health defects. Though genetically unrelated to frame or splash ... However, modern DNA testing has revealed that some breeds do possess genes for spotting patterns, such as a non-SB-1 sabino ... The word "pinto" is Spanish for 'painted', and also 'dappled' or 'spotted'.[1] ...
50 (1): 1-5. doi:10.1007/s000110050716. PMID 11235015.. *. Matsuoka Y, Furuyashiki T, Bito H, Ushikubi F, Tanaka Y, Kobayashi T ... "Entrez Gene: PTGER1 prostaglandin E receptor 1 (subtype EP1), 42kDa".. *↑ Woodward DF, Jones RL, Narumiya S (September 2011). " ... 228 (1): 23-30. doi:10.1111/j.1432-1033.1995.tb20223.x. PMID 7883006.. ...
Endothelin. *Agonists: Endothelin 1. *Endothelin 2. *Endothelin 3. *IRL-1620. *Antagonists: A-192621 ... Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... Integrin ligands (collagens, fibrinogen, fibronectin, laminins, ICAM-1, ICAM-2, osteopontin, VCAM-1, vitronectin) ...
Following apoptosis, it is thought there is a massive degranulation of vasoconstrictors, including endothelins and free ... endothelin receptor A and cyclin dependent kinase inhibitor. Mutations in interleukin 6 may be protective.[citation needed]. ... ISBN 978-1-934115-01-5.. *^ a b c DiMaio, Vincent J.; DiMaio, Dominick (2001). Forensic pathology (2nd ed.). Boca Raton, FL [ ... ISBN 0-7216-0187-1.. *^ a b c Brisman, JL; Song, JK; Newell, DW (Aug 31, 2006). "Cerebral aneurysms". The New England Journal ...
endothelin. ↑endothelin receptor ETA. angiotensin II. ↑Angiotensin receptor 1 *On smooth muscle cells: Activation of Gq --, ↑ ... ISBN 1-4160-2328-3.. Page 479 *^ a b c d e f g h i j Rod Flower; Humphrey P. Rang; Maureen M. Dale; Ritter, James M. (2007). ... ISBN 1-4160-2328-3.. Page 771 *^ Richard Milsten and Julian Slowinski, The sexual male, bc, main point W.W. Norton Company, New ... α1 adrenergic receptor Activation of Gq --, ↑PLC activity --, ↑IP3 and DAG --, activation of IP3 receptor in SR --, ↑ ...
Part I: Methodological issues for assessment in the different vascular beds: a statement by the Working Group on Endothelin and ... 23 (1): 7-17. doi:10.1097/00004872-200501000-00004. PMID 15643116.. *^ Roberts OL, Holmes K, Müller J, Cross DA, Cross MJ (Dec ... Endothelium refers to cells that line the interior surface of blood vessels and lymphatic vessels,[1] forming an interface ...
277 (1): 1-4. doi:10.1074/jbc.R100054200. PMID 11696554.. *^ a b c d Wooding S, Kim UK, Bamshad MJ, Larsen J, Jorde LB, Drayna ... 98 (1): 45-53. doi:10.1159/000068546. PMID 12584440.. *. Pronin AN, Tang H, Connor J, Keung W (2005). "Identification of ...
... endothelin-1, and thrombin.". Proc. Natl. Acad. Sci. U.S.A. 96 (4): 1633-8. PMC 15542. . PMID 9990076. doi:10.1073/pnas.96.4. ... 326 (1): 69-75. PMC 1218638. . PMID 9337852. الوسيط ,التاريخ=. تم تجاهله (مساعدة); الوسيط ,الصفحات=. تم تجاهله (مساعدة); الوسيط ... 1 (3): 201-7. PMC 3375599. . PMID 19138957. doi:10.1158/1940-6207.CAPR-08-0014. الوسيط ,السنة=. تم تجاهله (مساعدة); الوسيط , ... 24 (1): 176-84. PMID 18835871. doi:10.1093/humrep/den359. الوسيط ,السنة=. تم تجاهله (مساعدة); الوسيط ,الصفحات=. تم تجاهله ( ...
13 Suppl 1: S10-6. doi:10.1111/jth.12952. PMID 26149010.. *^ a b Kanaoka Y, Boyce JA (2014). "Cysteinyl leukotrienes and their ... 2003). "Expression and localization of the cysteinyl leukotriene 1 receptor in human nasal mucosa". Clin. Exp. Allergy. 32 (7 ... However, the first discovered receptor for these CsLTs, cysteinyl leukotriene receptor 1 (CysLTR1), appears to play the major ... 2005). "Expression of the cysteinyl leukotriene receptors cysLT(1) and cysLT(2) in aspirin-sensitive and aspirin-tolerant ...
Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor that in humans is encoded by the ... Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension. Inhibition of these receptors ... Han SG, Ko S, Lee WK, Jung ST, Yu YG (August 2017). "Determination of the endothelin-1 recognition sites of endothelin receptor ... Overview of all the structural information available in the PDB for UniProt: P05305 (Endothelin-1) at the PDBe-KB. This article ...
This enzyme catalyses the following chemical reaction Hydrolysis of the -Trp21-Val- bond in big endothelin to form endothelin 1 ... Endothelin-converting+enzyme+1 at the US National Library of Medicine Medical Subject Headings (MeSH) Biology portal v t e. ... Endothelin-converting enzyme 1 (EC 3.4.24.71, endothelin-converting enzyme, ECE-1) is an enzyme. ... Shimada K, Takahashi M, Tanzawa K (July 1994). "Cloning and functional expression of endothelin-converting enzyme from rat ...
The PDB archive contains information about experimentally-determined structures of proteins, nucleic acids, and complex assemblies. As a member of the wwPDB, the RCSB PDB curates and annotates PDB data according to agreed upon standards. The RCSB PDB also provides a variety of tools and resources. Users can perform simple and advanced searches based on annotations relating to sequence, structure and function. These molecules are visualized, downloaded, and analyzed by users who range from students to specialized scientists.
3 Abstracts with Endothelin-1 Inhibitor Research. Filter by Study Type. Animal Study. ... Pharmacological Actions : Anti-Inflammatory Agents, Endothelin-1 Inhibitor, Epidermal growth factor receptor (EGFR) inhibitor, ... Green tea extract suppresses the oxidative stress and endothelin-1 expression associated with pulmonary fibrosis.Sep 01, 2006. ... Black currant anthocyanins caused a normalization of serum levels of ET-1 and may slow down glaucoma progression.May 31, 2013. ...
Endothelin-1 receptor. P25101. Details. Drug Relations. Drug Relations. DrugBank ID. Name. Drug group. Pharmacological action? ... Endothelin-1 receptor. Kind. protein. Organism. Human. Polypeptides. Name. UniProt ID. ...
Plasma immunoreactive endothelin-1 in experimental malignant hypertension.. M Kohno, K Murakawa, T Horio, K Yokokawa, K ... Plasma immunoreactive endothelin-1 in experimental malignant hypertension.. M Kohno, K Murakawa, T Horio, K Yokokawa, K ... Plasma immunoreactive endothelin-1 in experimental malignant hypertension.. M Kohno, K Murakawa, T Horio, K Yokokawa, K ... We measured plasma concentrations of immunoreactive endothelin-1 (irET-1) in the prehypertensive and hypertensive phases in ...
Increased Endothelin-1 Levels of BAL Fluid in Patients with Behçets Disease. Kamel Hamzaoui,1 Hanene Chelbi,1 Mariam Kamoun,1 ... A. J. Peacock, K. E. Dawes, A. Shock, A. J. Gray, J. T. Reeves, and G. J. Laurent, "Endothelin-1 and endothelin-3 induce ... A. Giaid, R. P. Michel, D. J. Stewart, M. Sheppard, B. Corrin, and Q. Hamid, "Expression of endothelin-1 in lungs of patients ... L. Guembe and A. C. Villaro, "Immunohistochemical mapping of endothelin in the developing and adult mouse lung," Journal of ...
Use of the endothelin antagonists BQ-123 and PD 142893 to reveal three endothelin receptors mediating smooth muscle contraction ... Mechanisms of Big Endothelin-1-Induced Diuresis and Natriuresis. Role of ETB Receptors. Aaron Hoffman, Zaid A. Abassi, Sergey ... Endothelin, a peptide inhibitor of Na+-K+-ATPase in intact renal tubular epithelial cells. Am J Physiol. 1989;257:C1101-C1107. ... Analysis of responses to endothelins in isolated porcine blood vessels by using a novel endothelin antagonist, BQ-153. Life Sci ...
Endothelins are endothelium-derived vasoconstrictor peptides.; CSCSSLMDKECVYFCHLDIIWVNTPEHVVPYGLGSPRS (Disulfide bridge: 1-15 ... Big Endothelin-1 (1-38) is precursor of endothelin 1. Big endothelin-1 is cleaved to yield endothelin-1 via the activity of an ... endothelin-converting enzyme (ECE). Big Endothelin-1 can be hydrolyzed by chymase to generate endothelin 1 (1-21) in vitro. ... Big Endothelin-1 (1-38) is precursor of endothelin 1. Big endothelin-1 is cleaved to yield endothelin-1 via the activity of an ...
Previous studies in animal models indicated an autocrine/paracrine action of endothelin-1 (ET-1) in the ovary. We now report ... evidence on the presence of ET-1 in human ovary during reproductive life. Immunohistochemical and in situ hybridization studies ... Expression of endothelin-1 gene and protein in human granulosa cells J Clin Endocrinol Metab. 1996 Apr;81(4):1428-33. doi: ... Previous studies in animal models indicated an autocrine/paracrine action of endothelin-1 (ET-1) in the ovary. We now report ...
Mouse monoclonal Endothelin 1 antibody [TR.ET.48.5] validated for WB, IP, ELISA, IHC, RIA, Flow Cyt, Inhibition, ICC/IF and ... Anti-Endothelin 1 antibody [TR.ET.48.5] (ab2786) at 1/500 dilution + PC12 cell lysate at 25 µg. Predicted band size : 24 kDa. ... Nur77 attenuates endothelin-1 expression via downregulation of NF-?B and p38 MAPK in A549 cells and in an ARDS rat model.. Am J ... ab2786 labelling Endothelin 1 (green) in the secretion of HeLa cells (right) compared with a negative control (left) by ...
Characterization of endothelin receptors and effects of endothelin on diacylglycerol and protein kinase C in retinal capillary ... Nucleotide sequence of endothelin cDNA from bovine endothelial cells [14].. *To elucidate the cellular mechanism of endothelin- ... Regulation of endothelin 1 gene by fluid shear stress is transcriptionally mediated and independent of protein kinase C and ... Stimulation by endothelin-1 of mitogen-activated protein kinases and DNA synthesis in bovine tracheal smooth muscle cells. ...
The endothelin (ET) and prorenin/renin/prorenin receptor (PRR) systems have opposing physiological effects on collecting duct ( ... PRR knockout (KO) mice were polyuric and had markedly increased urinary ET-1 and inner medullary CD (IMCD) ET-1 mRNA. PRR KO ... Water loaded wild-type mice with similar polyuria as PRR KO mice had modestly increased urinary ET-1 excretion and inner ... medullary ET-1 mRNA, while inner medullary ETA and ETB mRNA or protein expression were unaffected. In contrast to PRR KO, CD ...
Endothelin-1 as a Potential Trigger of Migraine Aura. The safety and scientific validity of this study is the responsibility of ... Current animal evidence indicates that infusion of endothelin-1 (ET-1), a naturally occurring signaling molecule released from ... Investigations of the Endogenous Vasoconstrictor and Neuromodulator Peptide Endothelin-1 as a Potential Trigger of Migraine ... In this project the investigators aim to study the effects of ET-1 on the human brain, to investigate aura-inducing effects of ...
... and endothelin-3 (ET-3). All three isoforms are encoded by a 38-amino-acid precursor known as big endothelin. Endothelins are ... Endothelins are among the most potent vasoconstrictor proteins known. Overexpression of endothelins contributes to hypertension ... Anti-Human Big Endothelin-1 (22-38) Rabbit IgG Affinity Purify 5 ug $121.00 ... Anti-Rat Big Endothelin-1 (22-38) Rabbit IgG Affinity Purify 50 ug $529.00 ...
This led for the search for antagonists of endogenous endothelin and, more precisely, for an antagonist of endothelin-1 ... How can these normal plasma endothelin levels in hypertensive dogs be reconciled with a pathophysiological role of endothelin ... Pathophysiological role of endothelin revealed by the first orally active endothelin receptor antagonist. Nature. 1993;365:759- ... Effects of different endothelin receptor antagonists and of the novel non-peptide antagonist R0 46-2005 on endothelin levels in ...
Endothelin-1 Induces an Endothelin-A-Receptor-Dependent and L-NAME-Sensitive Vasoconstriction in the Isolated Perfused Guinea- ... Endothelin-1 (ET-1), IRL-1620, BQ-123, BQ-788, L-NAME, Vasoconstriction.. ... and ETB-receptors in the eicosanoid-releasing properties of endothelin-1 (ET-1) in the guinea-pig perfused lung. More recently ... Furthermore, the pressor effect of a dose of ET-1 (40 pmol) was markedly reduced after a 15-min infusion of the ETA antagonist ...
Endothelin-1 (ET-1) is an endogenous vasoconstrictor implicated in pulmonary and systemic hypertension, as well as ventricular ... Increased mortality with elevated plasma endothelin-1 in acute heart failure: an ASCEND-HF biomarker substudy.. Perez AL1, ... Median ET-1 was 7.6 [interquartile range (IQR) 5.9-10] pg/mL at baseline, 6.3 (IQR 4.9-8.1) pg/mL at 48-72 h, and 5.9 (IQR 4.7- ... Grodin JL1, Wu Y2, Hernandez AF3, Butler J4, Metra M5, Felker GM3, Voors AA6, McMurray JJ7, Armstrong PW8, Starling RC1, ...
Prospective Study on Plasma Pro-endothelin-1 in Predicting Bronchopulmonary Dysplasia. This study has been completed. ... Comparing pro-endothelin-1 with established clinical indices of bronchopulmonary dysplasia (BPD). Hypothesis: Pulmonary- ... Serial quantitative measurements of plasma pro-endothelin-1 concentrations in very preterm infants. ... vascular remodeling in infants developing BPD is directly related to circulating pro-endothelin-1, which therefore serves as ...
... endothelin-A (ETA) and endothelin-B (ETB)] mediating the characteristic vasoconstrictor response upon activation by the peptide ... Endothelin-1 (ET-1) content in lungs [n=5-12, as picograms per milligram (pg/mg) lung tissue] (A) of wild-type (WT) mice and ... Upregulation of endothelin receptor B in human endothelial cells by low-density lipoproteins. Exp Biol Med (Maywood) 2006; 231 ... Insulin stimulates endothelin-1 secretion from human endothelial cells and modulates its circulating levels in vivo. J Clin ...
Endothelin Receptor Expression. Thoracic aortic ETA Rc protein expression was significantly (P=0.004) increased after CyA ... Figure 3. Endothelin-1 (ET-1) plasma levels after 2 weeks of treatment. Rapamycin (SRL) treatment significantly reduces ET-1 ... Effects of cyclosporin A on the synthesis, excretion, and metabolism of endothelin in the rat. Hypertension. 1996; 27: 1140- ... Role Of Endothelin-1 and Nitric Oxide Bioavailability in Transplant-Related Vascular Injury. Comparative Effects of Rapamycin ...
D-Val22, Phe33] Big Endothelin-1 (16-38), Human, Alfa Aesar 1mg Life Sciences:Protein Biology:Proteins:Peptides:Catalog ... D-Val22, Phe33] Big Endothelin-1 (16-38), Human, Alfa Aesar ... D-Val22, Phe33] Big Endothelin-1 (16-38), Human, Alfa Aesar ...
Reduction in hepatic endothelin-1 clearance in cirrhosis Anh Thu TRAN DUC; Anh Thu TRAN DUC ... The Endothelin Family of Peptides: Local Hormones with Diverse Roles in Health and Disease? Clin Sci (Lond) (May, 1993) ... Circulating endothelin-1 (ET-1) levels are increased in cirrhosis. The liver is an important site for circulating ET-1 ... Anh Thu TRAN DUC, Andreas J. SCHWAB, André SIMARD, Louis VILLENEUVE, Jocelyn DUPUIS; Reduction in hepatic endothelin-1 ...
Endothelin-1 is a very powerful endogenous vasoconstrictor substance produced by endothelial cells. Its long-lasting ... 0/Azepines; 0/Endothelins; 0/Indoles; 0/Oligopeptides; 0/Peptides, Cyclic; 0/Receptors, Endothelin; 136553-81-6/cyclo(Trp-Asp- ... Availability of endothelin-1 antagonist provided a pharmacologic tool to test the role of endothelin in the development of ... Endothelins / metabolism*. Humans. Indoles / therapeutic use. Ischemic Attack, Transient / etiology, metabolism*, prevention & ...
... Proteomics. 2003 May;3(5):689-98. ... endothelin-1 stimulation of hypertrophy) and proteomic analysis to define a discrete set of differentially expressed proteins ... Gregory F Egnaczyk 1 , James D Pomonis, Julie A Schmidt, Scott D Rogers, Christopher Peters, Joseph R Ghilardi, Patrick W ... 1 Department of Pharmacology and Cell Biophysics, University of Cincinnati College of Medicine, Cincinnati, OH 45267, USA. ...
Endothelin-1: A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, ... Big Endothelin; Big Endothelin-1; ET-1 (Endothelin-1); Endothelin Type 1; Endothelin, Big; Preproendothelin; Preproendothelin-1 ... Endothelin-1 (Endothelin 1). Subscribe to New Research on Endothelin-1 A 21-amino acid peptide produced in a variety of tissues ... 07/01/2000 - "Big endothelin-1 (2.6+/-0.4 vs. 1. 7+/-0.1 pM; P=0.04) and C-terminal fragment immunoreactivity (2. 1+/-0.3 vs. ...
2012 Sep 15;691(1-3):218-24. doi: 10.1016/j.ejphar.2012.07.002. Epub 2012 Jul 13. Research Support, Non-U.S. Govt ... Expression of prepro-endothelin-1 (ppET-1) mRNA was determined by quantitative real time PCR. [(3)H]-Proline incorporation was ... Human lung fibroblasts are a potential source of endothelin-1 (ET-1), a pro-fibrotic mediator. The present study explored ... β₂-adrenoceptors and muscarinic receptors mediate opposing effects on endothelin-1 expression in human lung fibroblasts.. ...
MACRAE, I.M., ROBINSON, M.J., GRAHAM, D.I., REID, J.L. & McCULLOCH, J. (1993). Endothelin-1-induced reductions in cerebral ... ALLCOCK, G.H., WARNER, T.D. & VANE, J.R. (1995). Roles of endothelin receptors in the regional and systemic vascular responses ... TAKAHASHI, H., NAKANISHI, T., NISHIMURA, M., TANAKA, H. & YOSHIMURA, M. (1992). Effects of endothelin-1 and inhibition of ... Assessment of the effects of endothelin-1 and magnesium sulphate on regional blood flows in conscious rats, by the coloured ...
An animal model of capsular infarct: endothelin-1 injections in the rat. Behav Brain Res. 2006;169:206-11.PubMedCrossRefGoogle ... Focal lesions in the rat central nervous system induced by endothelin-1. J Neuropathol Exp Neurol. 2003;62:1276-86.PubMedGoogle ... Characterisation of Endothelin-1-Induced Intrastriatal Lesions Within the Juvenile and Adult Rat Brain Using MRI and 31P MRS. ... A new model of focal brain ischemia based on the intracerebral injection of endothelin-1. Ital J Neurol Sci. 1991;12:49-53. ...
Both Gsk3b-CKO mice and fibroblasts showed elevated expression and production of endothelin-1 (ET-1) compared with control mice ... GSK-3β in mouse fibroblasts controls wound healing and fibrosis through an endothelin-1-dependent mechanism. ... GSK-3β in mouse fibroblasts controls wound healing and fibrosis through an endothelin-1-dependent mechanism. ... Published October 1, 2008; First published September 18, 2008 Citation Information: J Clin Invest. 2008;118(10):3279-3290. ...
  • The protein encoded by this gene is proteolytically processed to release a secreted peptide termed endothelin 1. (wikipedia.org)
  • Preproendothelin is precursor of the peptide ET-1. (wikipedia.org)
  • Similar to A-192621.1, pretreatment with a nitric oxide synthase inhibitor (L-NAME, 10 mg/kg plus 5 mg · kg −1 · h −1 ) significantly and comparably reduced the diuretic and natriuretic actions of big ET-1 and augmented the hypoperfusion/hypofiltration and systemic vasoconstriction induced by high doses of the peptide. (ahajournals.org)
  • Pretreatment with verapamil (2 mg · kg −1 · h −1 ) slightly inhibited the diuretic/natriuretic effects of the high-dose big ET-1 and completely prevented the increase in mean arterial blood pressure provoked by the peptide. (ahajournals.org)
  • Background Endothelin-1, a vasoconstrictive peptide released by endothelium, may be involved in the pathophysiology of hypertension. (ahajournals.org)
  • Endothelin-1, a 21-amino-acid peptide produced by vascular endothelium, 1 is endowed with vasoconstrictive, inotropic, and mitogenic properties. (ahajournals.org)
  • 9 Since the discovery of endothelin-1, research has also focused on the potential roles of this peptide in some pathological states. (ahajournals.org)
  • By contrast to the similarly low plasma peptide levels in lean and obese wild type mice and littermates with heterozygous endothelial over-expression of the prepro-endothelin-1 gene (TET het ) 1 on standard chow or high fat diet, endothelin-1 levels in the lungs were significantly higher ( Figure 1A ). (nature.com)
  • Endothelin-1 acts via two distinct receptor subtypes [endothelin-A (ET A ) and endothelin-B (ET B )] mediating the characteristic vasoconstrictor response upon activation by the peptide of vascular smooth muscle cells 2 . (nature.com)
  • Therefore, the objective of the present study was to investigate the regional and subregional changes in haemodynamics in response to the vasoconstrictor peptide endothelin-1 (ET-1) and MgSO 4 in more detail, using the coloured microsphere reference technique. (wiley.com)
  • Endothelin-1 (ET-1) is a potent peptide vasoconstrictor that plays a significant role in regulating vascular homeostasis. (springer.com)
  • EDNRA encodes the bovine protein Endothelin-1 receptor (ETA), a peptide that plays a role in potent and long-lasting vasoconstriction. (cellsciences.com)
  • As Dr. Brody notes, increasing evidence supports endothelin-1 as an atherosclerotic peptide. (annals.org)
  • 1. We have investigated whether local vascular production of nitric oxide or prostacyclin regulates venoconstriction induced by the endothelium-derived peptide, endothelin-1, in vivo in man. (portlandpress.com)
  • The vascular endothelial cells have the ability to modulate local vascular tone by releasing relaxing factors such as nitric oxide or the vasoconstrictor peptide endothelin-1. (arvojournals.org)
  • Ln big ET-1 was positively associated with Ln N-terminal pro-brain natriuretic peptide, left ventricular diameter, but negatively related to age and Ln left ventricular ejection fraction. (onmedica.com)
  • The vasoactive peptide endothelin (ET)-1 attenuates sympathetic neurotransmission prejunctionally by decreasing nerve stimulation induced release of NE. (aspetjournals.org)
  • Cyclic stretch has been reported to enhance ET-1 peptide synthesis and prepro-ET-1 mRNA expression in cultured endothelial cells. (ahajournals.org)
  • Surprisingly, large amounts of mature ET-1 peptide are found in ECE-1−/− embryos, indicating that non-ECE-1 protease(s) can activate ET-1 at certain sites. (biologists.org)
  • However, endothelin-stimulated choline generation was greater than that observed in response to a protein kinase C-activating phorbol ester, raising the possibility that the peptide activates phospholipase D by both protein kinase C-dependent and -independent mechanisms. (biochemj.org)
  • Endothelin-1 (ET-1) is a 21-residue peptide originally isolated from supernatants of vascular endothelial cells. (ahajournals.org)
  • 1 ET-1 acts not only as a vasoconstrictive and growth-promoting peptide but also as a survival factor against apoptosis in smooth muscle cells, 2 fibroblasts, 3 and cardiac myocytes. (ahajournals.org)
  • Endothelin-1 (ET-1), a key mediator of inflammatory processes associated with gastric mucosal injury, is a potent vasoactive peptide produced from a biologically inactive big ET-1 by the action of endothelin-converting enzyme-1 (ECE-1). (brillonline.com)
  • We found similar concentrations of endothelin-1 in peripheral blood in multiple sclerosis patients and healthy controls, a higher endothelin-1 level in the upper part of right internal jugular veins, and unchanged concentrations of this peptide in peripheral blood following angioplasty. (termedia.pl)
  • It could be terminated by adding calcitonin-gene related peptide (CGRP), most likely because CGRP causes ET-1/ETAR dissociation. (eur.nl)
  • Endothelins are endothelium-derived vasoconstrictor peptides. (rcsb.org)
  • Endothelins (ETs) are a family of vasoconstrictive 21-amino acid peptides that are synthesized and released by endothelial cells that act in a paracrine/autocrine mode of action. (ahajournals.org)
  • 20 In addition, gene expression and immunoreactive peptides of ET-1 21 22 and its receptors have been demonstrated in the renal tissue, especially in the medullary region. (ahajournals.org)
  • The antibodies were raised in rabbit using synthetic big ET-1 (22-38) peptides, and can be used for immunohistochemical (IHC) detection of human or rat big ET-1 protein. (clontech.com)
  • The Endothelin Family of Peptides: Local Hormones with Diverse Roles in Health and Disease? (portlandpress.com)
  • ET-1 and Ang II are two potent vasoactive peptides that have an extensive tissue distribution, including the heart. (ahajournals.org)
  • Stjernquist M (1998) Endothelins-vasoactive peptides and growth factors. (springer.com)
  • Edn1 is one of three known Endothelin peptides, each synthesized as a larger prepropeptide and subsequently modified by furin proteases and endothelin converting enzymes (ECEs) to form a mature ligand. (biologists.org)
  • Vasopressin, endothelin and adrenomedullin are vasoactive peptides that regulate vascular tone and might play a role in hypertensive diseases. (uzh.ch)
  • Abstract -Endothelin-1 (ET-1) at high concentrations has marked antidiuretic and antinatriuretic activities, whereas its precursor, big endothelin-1 (big ET-1), has surprisingly potent diuretic and natriuretic actions. (ahajournals.org)
  • Abstract This study investigates the cellular localization and regulation of endothelin-1 (ET-1) and angiotensin II (Ang II) receptors and the effects of ET-1 and Ang II on [Ca 2+ ] i in cardiac hypertrophy due to volume overload in the rat. (ahajournals.org)
  • Abstract -Upregulation of endothelin-1 (ET-1) synthesis in venous bypass grafts in response to arterial levels of blood pressure may play a major role in graft failure. (ahajournals.org)
  • Endothelin 1 (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor that in humans is encoded by the EDN1 gene and produced by vascular endothelial cells. (wikipedia.org)
  • Substantial efforts have led to the identification of several genes required for craniofacial skeletal development such as the endothelin-1 (edn1) signaling pathway that is required for lower jaw formation. (mit.edu)
  • To test this hypothesis, we analyzed data from HyperPATH - 1,788 individuals from the total cohort and 765 restricted to ED-to-AD in a 2:1 match and genotyped for the endothelin-1 gene (EDN1). (jci.org)
  • Genetic studies in mice and zebrafish have revealed conserved requirements for Endothelin 1 (Edn1) signaling in craniofacial development. (biologists.org)
  • EDN1, also named as Endothelin-1, PPET1 and ET-1, belongs to the endothelin/sarafotoxin family. (ptglab.com)
  • 1 2 3 4 The mature ET-1 activates 2 subtypes of receptors, ET A and ET B . 5 6 The activation of the ET A receptor, which is located in vascular smooth muscle cells, increases intracellular Ca 2+ , leading to prolonged vasoconstriction. (ahajournals.org)
  • 9 10 11 12 13 ET B receptors have also been described in certain smooth muscle cells of vascular beds and may contribute under certain circumstances to ET-1-mediated vasoconstriction. (ahajournals.org)
  • 1 2 3 4 5 Exogenous administration of endothelin-1 results in a biphasic response characterized by a transient vasodilation followed by a sustained vasoconstriction. (ahajournals.org)
  • 6 This response has been attributed to stimulation of two subtypes of endothelin receptors: the ET A receptor, mediating vasoconstriction, and the ET B receptor, causing endothelium-dependent vasodilation (through a release of endothelium-derived relaxing factor [EDRF] and/or prostacyclin). (ahajournals.org)
  • The ET-1-induced vasoconstriction was restored 50 min after the cessation of BQ-123 infusion. (lww.com)
  • We suggest that local production of ET-1 by neutrophils and other inflammatory cells could be a molecular sign of focal inflammation in histologically normal appendixes and that ET-1 could be implicated, with other cytokines, in the pathogenesis of appendicitis by inducing appendiceal ischemia through vasoconstriction. (physiology.org)
  • High ET-1 immunoreactivity has been shown in lamina propria and submucosa of patients with Crohn's disease and ulcerative colitis ( 19 ), and it has been suggested that local endothelin production by inflammatory cells may contribute to vasculitis in chronic inflammatory bowel disease by inducing intestinal ischemia through vasoconstriction ( 19 ). (physiology.org)
  • 10 - 14 Previously, we also reported that ET-1 plays a major role in hyperoxia-induced vasoconstriction in cats. (arvojournals.org)
  • ET-1) is the most potent vasoconstriction agent known and its serum levels are increased in PIH. (srce.hr)
  • The endothelin system has recently been demonstrated to regulate oxygen availability in the diabetic kidney via a pathway involving endothelin type A receptors (ETA-R). These receptors mainly mediate vasoconstriction and tubular sodium retention, and inhibition of ETA-R improves intrarenal oxygenation in the diabetic kidney. (physiology.org)
  • When added on top of ET-1-initiated contraction in RMA, CGRP effectively counteracted vasoconstriction, i.e., it caused full relaxation. (eur.nl)
  • Endothelin-1 (ET-1) is an endogenous vasoconstrictor implicated in pulmonary and systemic hypertension, as well as ventricular dysfunction, through effects on vascular smooth muscle, the kidneys, and cardiomyocytes. (nih.gov)
  • Hypothesis: Pulmonary-vascular remodeling in infants developing BPD is directly related to circulating pro-endothelin-1, which therefore serves as surrogate marker of BPD. (clinicaltrials.gov)
  • We have published in this journal a study investigating comprehensively the vascular responses in a mouse model of heterozygous endothelial overexpression of the endothelin-1 gene concluding that the latter in combination with obesity aggravates renal arterial dysfunction 1 . (nature.com)
  • Endothelin-1 contributes to increased vascular reactivity and tone under cardiovascular risk conditions including obesity in both humans and animal models 2 . (nature.com)
  • This may occur despite an augmented ET B -receptor mediated increase in vascular tone as seen in some peripheral arteries from obese animals, in particular in those of endothelin-1 gene overexpressing mice 1 and contribute to the less than expected vascular and metabolic phenotype. (nature.com)
  • Although alterations in ET-1 system components are observed in some studies, there remains a need for future research to clarify whether these specific changes are compensatory or causally related to vascular injury and dysfunction. (springer.com)
  • 1 Although the exact interplay of mechanisms leading to glaucoma remains a subject of investigation, it is believed that elevated intraocular pressure (IOP), vascular dysregulation, and alterations in numerous substances of the intraocular milieu are involved. (dovepress.com)
  • Antisense oligodeoxynucleotides to endothelin ETA receptor mRNA were used to characterize vascular smooth muscle receptors. (lu.se)
  • 15 Endothelin-1 is a 21 amino acid polypeptide, expressed in both endothelial and glial components in the retina, 16 that has a potent constrictor action by binding to the high-affinity ET type A (ETA) receptor in retinal vascular smooth muscle cells and pericytes. (arvojournals.org)
  • These findings demonstrate that in the human ophthalmic artery, endothelium-derived nitric oxide and endothelin are very potent modulators of vascular tone, suggesting that they play an important role in the regulation of local blood flow in the eye. (arvojournals.org)
  • The endothelium regulates vascular tone and growth by releasing such factors as nitric oxide and endothelin-1. (annals.org)
  • Naftidrofuryl (Naf) (marketed under the trade name Praxilene) improves walking distance in patients with peripheral vascular disease, an effect which may be partially attributed to ET-1 antagonism. (clinsci.org)
  • Off-pump myocardial revascularization attenuates ET-1 expression in all investigated vascular compartments. (springermedizin.at)
  • Cholesterol depletion impairs vascular reactivity to endothelin-1 by reducing store-operated Ca2+ entry dependent on TRPC1. (lu.se)
  • The reactivity of the vascular wall to endothelin-1 (ET-1) is influenced by cholesterol, which is of possible importance for the progression of atherosclerosis. (lu.se)
  • These results suggest that cholesterol influences vascular reactivity to ET-1 by affecting the caveolar localization of TRPC1. (lu.se)
  • COX-2 inhibitors and, in part, COX-1 inhibitor blocked ET-1-induced PGE 2 and vascular endothelial growth factor release, indicating that both enzymes participate in PGE 2 production to a different extent. (aacrjournals.org)
  • Endothelin-1, angiotensin II and neuropeptide-Y all reduced common and internal carotid vascular conductance and this effect was significantly attenuated by low dose MgSO 4 . (clinsci.org)
  • It has been shown that NO antagonizes the action of ET-1 in vascular smooth muscle cells ( Rizvi and Myers, 1997 ). (aspetjournals.org)
  • Furthermore, acute hypertension induced by angiotensin II or phenylephrine did not affect the plasma irET-1 concentration in rats. (ahajournals.org)
  • The serine protease chymase has been reported to generate intracardiac angiotensin-II (Ang-II) from Ang-I as well as an intermediate precursor of endothelin-1 (ET-1), ET-1 (1-31) from Big-ET-1. (sigmaaldrich.com)
  • 4 Several lines of evidence based on cardiac expression of preproET-1 gene, 4 8 9 as well as renin, angiotensinogen, and angiotensin-converting enzyme genes, 10 11 suggest the existence of a local ET production and a local renin-angiotensin system in the myocardium. (ahajournals.org)
  • Autoantibodies to angiotensin and endothelin receptors in systemic sclerosis induce cellular and systemic events associated with disease pathogenesis. (bmj.com)
  • 3. After a period of recovery the animals were infused with endothelin-1, angiotensin II, neuropeptide-Y or N G -nitro- l -arginine methyl ester alone or in combination, and MgSO 4 in low or high dose was infused when the effects of the vasoconstrictors had become established. (clinsci.org)
  • Endothelins are among the most potent vasoconstrictor proteins known. (clontech.com)
  • By contrast, intrastriatal microinjection of the potent vasoconstrictor, endothelin-1 (ET-1), induces a focal, reversible and low-flow ischaemia in the absence of a typical inflammatory response, which gradually restores blood flow over several hours and may be more relevant to TIA and AIS pathology. (springer.com)
  • Endothelin-1 (ET-1) is the most potent vasoconstrictor in the body. (dovepress.com)
  • The potent vasoconstrictor endothelin-1 (ET-1) is at its highest concentration in the normal human ejaculate and is associated with the progression of metastatic prostate cancer. (aacrjournals.org)
  • In this pilot study we examined the potent vasoconstrictor, endothelin-1, in the blood of multiple sclerosis patients in the context of chronic cerebrospinal venous insufficiency hypothesis. (termedia.pl)
  • Endothelin-converting enzyme 1 (EC 3.4.24.71, endothelin-converting enzyme, ECE-1) is an enzyme. (wikipedia.org)
  • This enzyme catalyses the following chemical reaction Hydrolysis of the -Trp21-Val- bond in big endothelin to form endothelin 1 This metalloendopeptidase belongs to the peptidase family M13. (wikipedia.org)
  • 1 ET-1, the principal isoform of the ET family, is generated through a unique proteolytic cleavage of its precursor, big ET-1 (38 or 39 amino acids), by a specific phosphoramidon-sensitive metalloprotease called ET-converting enzyme (ECE). (ahajournals.org)
  • Big endothelin-1 is cleaved to yield endothelin-1 via the activity of an endothelin-converting enzyme (ECE). (anaspec.com)
  • Plasma ET-1 concentrations were determined using a commercially available enzyme-linked immunosorbent assay kit. (dovepress.com)
  • To examine if endothelin-converting enzyme-1 (ECE-1), as an ET-1-generating enzyme located in retinal glial cells, immunohistochemical examinations with costaining of antiglial fibrillary acidic protein (GFAP) antibody and anti-ECE-1 antibody were performed in whole-mount retinas. (arvojournals.org)
  • As judged by reverse transcription-polymerase chain reaction analysis (mRNA level), neither endothelin-converting enzyme nor endothelin A receptor expression appeared to be pressure sensitive. (ahajournals.org)
  • It is derived from a 212-amino acid precursor, prepro-ET-1, that is sequentially processed to big ET-1 and ET-1 by a furin-like protease and an endothelin-converting enzyme (ECE-1). (ahajournals.org)
  • Plasma endothelin (ET) concentrations were detected using an enzyme immunoassay. (molvis.org)
  • Values of ET-1 were compared between groups at all time points and correlated with postoperative cardioselective enzyme values and clinical parameters. (springermedizin.at)
  • Endothelin converting enzyme-1 (ECE-1) catalyzes the proteolytic activation of big endothelin-1 to endothelin-1(ET-1) in vitro. (biologists.org)
  • Endothelin-converting enzyme (ECE-1) is a type II integral membrane protein which plays a key role in the biosynthetic pathway of the vasoconstricting endothelins. (biologists.org)
  • Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension. (wikipedia.org)
  • Increased Plasma Endothelin-1 in Pulmonary Hypertension: Marker or Mediator of Disease? (annals.org)
  • The higher level of serum Endothelin and expression of ET-1 and ETA in broiler lungs may explain the higher sensitivity of broilers to the vasoconstrictions activity of endothelin and the higher sensitivity of these animals to pulmonary hypertension (PH). (magiran.com)
  • Placenta growth factor and endothelin in sickle cell pulmonary hypertension / Gregory J. Kato. (nih.gov)
  • Endothelin-1 Induces an Endothelin-A-Receptor-Dependent and. (lww.com)
  • Exogenous ET-1 induces prostate cancer proliferation directly and enhances the mitogenic effects of insulin-like growth factor I, insulin-like growth factor II, platelet-derived growth factor, basic fibroblast growth factor, and epidermal growth factor in serum-free conditions in vitro . (aacrjournals.org)
  • ET-1 also induces impairment of mucosal microvascular perfusion through activation of ET A receptors, causing significant tissue injury in the rat small intestine ( 17 ). (physiology.org)
  • ET-1 also induces NO release via iNOS induction. (umontreal.ca)
  • ET-1 induces cardiac gene transcription and protein expression of antiapoptotic B cell leukemia-2 (bcl-2) in a calcineurin-dependent manner. (ahajournals.org)
  • It remains to be determined whether ET-1 induces NO production in cardiomyocytes and whether intracellular NO could modulate ET-1-induced cardiomyocyte hypertrophic response, including the induction of early response gene and re-expression of fetal gene program. (aspetjournals.org)
  • Pulmonary fibrosis and chronic lung inflammation in ET-1 transgenic mice," American Journal of Respiratory Cell and Molecular Biology , vol. 23, no. 1, pp. 19-26, 2000. (hindawi.com)
  • Published in print September 1, 2000. (diabetesjournals.org)
  • We measured plasma concentrations of immunoreactive endothelin-1 (irET-1) in the prehypertensive and hypertensive phases in spontaneously hypertensive rats (SHR) and in malignant hypertension caused by deoxycorticosterone acetate (DOCA)-salt administration in SHR. (ahajournals.org)
  • Plasma irET-1 concentrations in young (6-week-old) and mature (18-week-old) SHR did not differ from those of age-matched Wistar-Kyoto (WKY) rats. (ahajournals.org)
  • Four weeks of treatment with DOCA-salt increased blood pressure, blood urea nitrogen, serum creatinine, and plasma irET-1 in SHR but not in WKY rats. (ahajournals.org)
  • Plasma irET-1 concentrations were not increased in the 2K1C rats. (ahajournals.org)
  • Six weeks of caffeine administration increased blood pressure, blood urea nitrogen, serum creatinine, plasma renin activity, and plasma irET-1 in the 2K1C rats but not in the sham-operated rats. (ahajournals.org)
  • High-performance liquid chromatographic profiles of plasma extracts pooled from these rats with malignant hypertension showed that a major component of irET-1 eluted in the position of synthetic ET-1 (1-21). (ahajournals.org)
  • To explore these mechanisms, we examined the effects of a highly selective ET B antagonist (A-192621.1), a calcium channel blocker (verapamil), a nitric oxide synthase inhibitor ( N -nitro- l -arginine methyl ester [L-NAME]), and a cyclooxygenase inhibitor (indomethacin) on the systemic and renal actions of big ET-1 in anesthetized rats. (ahajournals.org)
  • In the present study, the role of endothelin-1 (ET-1) on alterations of hepatic and renal metallothionein (MT) and trace metals (Zn, Cu, and Fe) were investigated in streptozotocin (STZ)- induced diabetic rats. (hindawi.com)
  • Hepatic and renal ET-1 mRNA was increased in diabetic rats as compared to control rats, along with an increase in both hepatic and renal MT proteins. (hindawi.com)
  • This study determined the temporal and spatial profile of NADPH oxidase subunit expression/activity concurrently with angiogenesis in the brain following transient ischemic stroke induced by prolonged constriction of the middle cerebral artery by perivascular injection of endothelin-1 in conscious Hooded Wistar rats ( n = 47). (mdpi.com)
  • 0.78 pmol h-1 directly into the renal artery) on kidney function and oxygen metabolism were investigated in normoglycemic controls and insulinopenic male Sprague Dawley rats administered streptozotocin (55 mg kg-1) two weeks before the acute experiments. (physiology.org)
  • Andrzejewska A, Dlugosz JW, Augustynowicz A. Effect of endothelin-1 receptor antagonists on histological and ultrastructural changes in the pancreas and trypsinogen activation in the early course of caerulein-induced acute pancreatitis in rats. (wjgnet.com)
  • Table 1 Histological changes in the pancreas of rats with caerulein-induced acute pancreatitis (AP) in comparison to control group (C), SE range of scores in brackets. (wjgnet.com)
  • In vivo prevention of ET-1-induced sudden death in 6 rats by pretreatment with endothelin receptor antagonist at a dose of 30 mg/kg p.o. (nih.gov)
  • In separate experiments rats were given compound 48/80 (50 µg·kg−1) to compare the effects of ET-1 with those of a known mast cell degranulator. (strath.ac.uk)
  • In the current study, male Sprague Dawley rats were subjected to endothelin-1 induced stroke. (deepdyve.com)
  • In primary cardiac myocytes prepared from neonatal rats, mutation of 2 NFAT sites within the bcl-2 promoter completely abolished the ET-1- and p300-induced increases in the activity of this promoter. (ahajournals.org)
  • Finally, a 60 min infusion with the nitric oxide synthase inhibitor, L-NAME (200 μM) markedly potentiated the constrictor effects of ET-1. (lww.com)
  • We studied variants in BMPR2, endothelin-1 (ET-1) and nitric oxide synthase 2 (NOS2). (ersjournals.com)
  • The levels of nitric oxide synthase (NOS), Endothelin 1 (ET-1) and β-actin transcripts were determined by real-time reverse transcriptase (RT)-PCR. (magiran.com)
  • The expression of endothelin 1 (ET-1) and nitric oxide synthase (NOS) genes in the heart and lung of broiler chickens has been affected by feeding Urtica dioica to broiler chickens. (magiran.com)
  • Belongs to the endothelin/sarafotoxin family. (abcam.com)
  • Plasma immunoreactive endothelin-1 in experimental malignant hypertension. (ahajournals.org)
  • The results suggested that the plasma ET-1 concentration is increased in rat models of malignant hypertension and that the high blood pressure itself is not the main factor involved in the increase of plasma ET-1. (ahajournals.org)
  • Overexpression of endothelins contributes to hypertension and heart disease. (clontech.com)
  • The goal of the present study was to evaluate the role of endogenous endothelin-1 in renal hypertension in dogs. (ahajournals.org)
  • Conclusions Specific endothelin-1 receptor antagonism markedly lowers blood pressure in experimental hypertension but is less effective on blood pressure of healthy animals. (ahajournals.org)
  • This suggests that endothelin-1 plays a role in the pathophysiology of hypertension but contributes to a lesser extent to the maintenance of normal blood pressure. (ahajournals.org)
  • Although it is clear that endothelin-1 is involved in the pathophysiology of conditions such as myocardial ischemia, 10 11 cyclosporine nephrotoxicity, 12 13 and subarachnoid hemorrhage-induced vasospasm, 14 15 it is questionable whether endothelin-1 would play a role in arterial hypertension. (ahajournals.org)
  • Reports on plasma endothelin-1 concentrations in hypertension have been controversial, as they were found to be either normal or slightly elevated. (ahajournals.org)
  • It has been reported that the production and function of ET-1 and its receptors are upregulated in a number of disease states associated with endothelium dysfunction including hypertension and atherosclerosis. (springer.com)
  • Background Endothelin-1 type A receptor (ETAR) antagonists (e.g. ambrisentan) are currently approved by the U.S Food and Drug administration, representing a well-tolerated treatment of pulmonary arterial hypertension (PAH)[1] for patients with connective tissue diseases such as systemic sclerosis (SSc). (bmj.com)
  • In this model of hypertension, ET-1 is a major activator of collagen I formation in renal resistance vessels and participates in the development of renal fibrosis without affecting systolic blood pressure. (ovid.com)
  • Plasma endothelin-1 levels, similar under basal conditions in healthy and hypertensive dogs, increased 30-fold with bosentan ( P =.0001). (ahajournals.org)
  • Correlation between plasma endothelin-1 levels and severity of septic liver failure quantified by maximal liver function capacity (LiMAx test). (plos.org)
  • This led for the search for antagonists of endogenous endothelin and, more precisely, for an antagonist of endothelin-1 receptors. (ahajournals.org)
  • Furthermore, the pressor effect of a dose of ET-1 (40 pmol) was markedly reduced after a 15-min infusion of the ETA antagonist, BQ-123 (1 μM). (lww.com)
  • Indomethacin (5 μM) and the ETB-receptor antagonist, BQ-788 (10 nM) did not affect the constrictor effect of ET-1. (lww.com)
  • Kinetic modelling revealed a major irreversible binding site for ET-1 that is blocked by the selective ET B receptor antagonist BQ788 and a minor non-specific reversible binding site that cannot be blocked with BQ788 or the selective ET A antagonist BQ123. (portlandpress.com)
  • Availability of endothelin-1 antagonist provided a pharmacologic tool to test the role of endothelin in the development of vasospasm. (biomedsearch.com)
  • Muscarinic agonist-induced stimulation of [(3)H]-proline incorporation was attenuated by the endothelin ET1 receptor antagonist bosentan. (nih.gov)
  • ET B R blockade with the specific antagonist, BQ788, inhibits in vitro and in vivo ET-1-induced effects, demonstrating that ET-1 through ET B R directly regulates lymphatic vessel formation and by interacting with the HIF-1α-dependent machinery can amplify the VEGF-mediated lymphatic vascularization. (aacrjournals.org)
  • The ET A -selective receptor antagonist A-127722 inhibits ET-1-stimulated growth, but the ET B -selective receptor antagonist BQ-788 does not. (aacrjournals.org)
  • Complementary experiments with the selective endothelin ETA receptor antagonist FR139317 demonstrated a shift of the concentration-response curve to the right in a competitive manner (pA2 = 6.93). (lu.se)
  • In contrast, endothelin-1 evoked potent contractions, which were unaffected by the calcium antagonist nifedipine. (arvojournals.org)
  • 17 18 The ET A subtype binds with high-affinity ET-1 and ET-2 but not ET-3 and may be selectively blocked by the ET antagonist BQ123. (ahajournals.org)
  • In addition, ET-1 was added to the detrusor strips in the presence of the ET A antagonist, BQ123, and the ET B antagonist, BQ788, to identify the receptor subtype functionally involved. (clinsci.org)
  • LU 302872 (non-selective ET-1 receptor A and B antagonist) or LU 302146 (selective ET-1 receptor A antagonist) were given i.p . at the indicated dosage at the beginning of the experiment, at 0 time, simultaneously with the first i.p . injection of caerulein. (wjgnet.com)
  • Endothelin-1 causes long-lasting contraction via endothelin type A receptor (ETAR) in isolated rat mesenteric arteries (RMA) that cannot be readily terminated by removing the agonist, or by adding the ETAR antagonist BQ123 or the NO donor sodium nitroprusside. (eur.nl)
  • Thus, in addition to the reported dissociation of ET-1/ETAR complexes, CGRP causes long-lasting non-selective arterial smooth muscle relaxation that may add to the neuropeptide being a physiological antagonist of arterial effects of ET-1. (eur.nl)
  • Endothelin-1 (ET-1) content in lungs [ n =5-12, as picograms per milligram (pg/mg) lung tissue] (A) of wild-type (WT) mice and littermates with heterozygous endothelial overexpression of the endothelin-1 gene (TET het ) on standard chow (lean) and after 30 weeks of high fat feeding (obese). (nature.com)
  • The hypertrophic response is characterized by increased cardiomyocyte cell volume, proliferation of nonmyocyte cells (mainly fibroblasts), activation of the fetal gene expression (myosin light chain 2, skeletal α-actin, β-myosin heavy chain, ANP, and BNP) and proto-oncogenes, 1 and altered [Ca 2+ ] i regulation. (ahajournals.org)
  • For ET-1 gene the polymorphism K198N was selected because homozygous for Asn (T/T genotype) have higher levels of ET-1. (ersjournals.com)
  • K198N (G/T) polymorphism in ET-1 gene showed similar distribution. (ersjournals.com)
  • Treatment of the segments with actinomycin D (1 μmol/L), the specific protein kinase C inhibitor, Ro 31-8220 (0.1 μmol/L), or the c-Src family-specific tyrosine kinase inhibitor, herbimycin A (0.1 μmol/L), demonstrated that the pressure-induced expression of these gene products occurs at the level of transcription and requires activation of protein kinase C, but not c-Src. (ahajournals.org)
  • In venous bypass grafts such deformation-induced changes in gene expression may contribute not only to acute graft failure through ET-1-induced vasospasm but also to endothelin A receptor- and/or endothelin B receptor-mediated smooth muscle cell hyperplasia and graft occlusion. (ahajournals.org)
  • To investigate whether a pressure-induced increase in tensile strain also affects prepro-ET-1 gene expression in the vessel wall in situ, we have developed an experimental model in which isolated segments of the rabbit external jugular vein are perfused at different levels of intraluminal pressure. (ahajournals.org)
  • To analyze the frequency of polymorphic variants of the endothelin EDN gene (K198N) and the endothelin receptor type A gene EDN RA (C1222T, C70G, G231A), DNA was isolated from peripheral blood, and SNP genotyping was performed using the real-time PCR (RT-PCR) method. (molvis.org)
  • NOS gene has been highly over expressed in the heart and lung of broilers fed Urtica dioica from 1 to 1.5 % increase relative to the control. (magiran.com)
  • Recent gene targeting studies have revealed unexpected roles for endothelins in the development of neural crest-derived tissues. (biologists.org)
  • Here we generated a targeted null mutation in the mouse ECE-1 gene. (biologists.org)
  • We observed a mild increase in HIF-1 and its target gene, glucose transporter-1. (deepdyve.com)
  • These findings suggest that ET-1-dependent NFATc signaling associates with p300 in the transactivation of bcl-2 gene in cardiac myocytes. (ahajournals.org)
  • 5,8 The calcineurin/NFATc pathway not only mediates changes in gene expression during cardiac hypertrophy 9 but also is required for ET-1- and phenylephrine-mediated protection against myocardial cell apoptosis. (ahajournals.org)
  • 5 However, the precise mechanisms by which ET-1-dependent signaling transactivates the bcl-2 gene in cardiac myocytes are unknown. (ahajournals.org)
  • The ET-1-stimulated activator protein-1 (AP-1) DNA binding activity and AP-1-mediated reporter activity were attenuated by NO. In addition, NO also significantly inhibited ET-1-stimulated promoter activity of hypertrophic marker gene β-myosin heavy chain and the enhanced protein synthesis. (aspetjournals.org)
  • The released NO consequently attenuated ET-1-induced c- fos gene expression through cGMP-mediated suppression of the ERK signaling pathway. (aspetjournals.org)
  • Three ECE-1 isoforms, differing by their N-terminal cytoplasmic tails, are generated from a single gene. (biologists.org)
  • Pretreatment with A-192621.1 (3 mg/kg plus 3 mg · kg −1 · h −1 ) significantly abolished the diuretic (17±5 μL/min to a maximum of 19±3 μL/min) and natriuretic (0.29±0.1% to a maximum of 1.93±0.37%) responses induced by big ET-1. (ahajournals.org)
  • We studied the influence of pretreatment with endothelin-1 on cardiac baroreflexes and on the effect of clonidine on blood pressure and heart rate. (frontiersin.org)
  • Endothelin pretreatment, either 50 ng/kg centrally or peripherally, had no significant effect on the hypotension or bradycardia produced either by central or peripheral injection of clonidine. (frontiersin.org)
  • Contractions induced by 10 nM endothelin-1 (ET) in the rabbit aortic media intimal layer were inhibited by prior exposure to 100 microM Ni++ (33.1%) or to a Ca(++)-free buffer (80.2%) but were unaffected by pretreatment with 0.1 microM nifedipine. (aspetjournals.org)
  • In this study, we investigated gastric mucosal expression of ECE-1 during a 16 h course of inflammatory responses associated with gastric mucosal damage caused by indomethacin, and evaluated the effect of pretreatment with an antiulcer agent, sucralfate, on this process. (brillonline.com)
  • Moreover, the reduction in the severity of damage following pretreatment with sucralfate was reflected at the end of 16-h period in a 47.4% decrease in the mucosal expression of TNF- α , 25.1% decline in ET-1, and a 38.9% decline in apoptosis. (brillonline.com)
  • Big Endothelin-1 (1-38) is precursor of endothelin 1. (anaspec.com)
  • All three isoforms are encoded by a 38-amino-acid precursor known as big endothelin. (clontech.com)
  • Full length protein corresponding to Human Endothelin 1 conjugated to Keyhole Limpet Haemocyanin (KLH). (abcam.com)
  • These kits can be used to measure soluble human or rat big ET-1 protein in serum, EDTA-plasma, cell culture supernatants, or tissue extracts. (clontech.com)
  • SRL did not impair Edep vasorelaxation or increase sensitivity to vasospasm while lowering ET-1 levels and preserving eNOS protein expression. (ahajournals.org)
  • To begin to understand the alterations in astrocyte protein expression that drive glial changes that occur following injury, we used an established model system (endothelin-1 stimulation of hypertrophy) and proteomic analysis to define a discrete set of differentially expressed proteins and post-translational modifications that occur as the astrocytes change from a quiescent to a reactive state. (nih.gov)
  • This orchestrated set of changes included proteins involved in cytoskeletal reorganization (caldesmon, calponin, alpha B-crystallin, stathmin, collapsing response mediator protein-2), cell adhesion (vinculin, galectin-1), signal transduction (RACK-1) and astrocyte differentiation (glutamine synthetase). (nih.gov)
  • The ETA receptor is a member of the endothelin receptor group of G-protein-coupled receptors that also includes ETB. (cellsciences.com)
  • The endothelin (ET) axis is composed of three isopeptides namely ET-1, ET-2, and ET-3 and two G-protein coupled receptors, ET A receptor (ET A R) and ET B R, which are expressed in endothelial cells, tumor cells, fibroblasts, and macrophages ( 11 ). (aacrjournals.org)
  • ET-1 protein expression is detected in situ in 14 of 14 primary cancers and 14 of 16 metastatic sites of human prostatic carcinoma. (aacrjournals.org)
  • The cells were isolated from human articular cartilage obtained at surgery and were cultured in the absence or presence of ET-1 with or without inhibitors of protein kinase or LY83583 (an inhibitor of soluble guanylate cyclase and of cGMP). (umontreal.ca)
  • Similarly, the ET-1-induced NO production was partially suppressed by the p38 kinase inhibitor and was completely suppressed by the protein kinase A kinase inhibitor KT5720 and by LY83583, suggesting the involvement of these enzymes in relevant ET-1 signalling pathways. (umontreal.ca)
  • These data suggest that ET-1 modulates the release of ATP via the ET B receptor and its associated G i/o G-protein through attenuation of the influx of extracellular Ca 2+ through L-type channels. (aspetjournals.org)
  • In contrast, there was a profound and time-dependent increase in endothelial prepro-ET-1 mRNA and intravascular ET-1 abundance (by ELISA) as well as in smooth muscle endothelin B receptor mRNA and functional protein (by superfusion bioassay) on raising the perfusion pressure from 5 to 20 mm Hg, but not from 0 to 5 mm Hg, for up to 12 hours. (ahajournals.org)
  • Endothelin-1 is known as a secretory protein presented in various types of brain cells, which has been indicated as a factor for cancer pathology. (springer.com)
  • The endothelin-1-induced cell migration was attenuated by MMP-9 and MMP-13 inhibitors and inhibitors of mitogen-activated protein (MAP) kinase and PI3 kinase/Akt. (springer.com)
  • Furthermore, the elevated levels of phosphate c-Jun accumulation in the nucleus and activator protein-1 (AP-1)-DNA binding activity were also found in endothelin-1 treated glioma cells. (springer.com)
  • The endothelin-stimulated increase in choline generation was abolished in cells where protein kinase C was down-regulated. (biochemj.org)
  • These stimuli bind to heterotrimeric G protein-coupled receptors and rapidly activate immediate-early genes (c- fos , c- jun, egr-1 , etc.) that encode transcription factors via protein kinase C (PKC) pathway and mitogen-activated protein kinase (MAPK) phosphorylation cascade ( Bueno and Molkentin, 2002 ). (aspetjournals.org)
  • Glomerular filtration rate and renal plasma flow significantly decreased only at the highest dose of big ET-1. (ahajournals.org)
  • Moreover, A-192621.1 potentiated the decline in glomerular filtration rate and renal plasma flow and the increase in mean arterial blood pressure produced by the low doses of big ET-1. (ahajournals.org)
  • Unlike verapamil and L-NAME, only indomethacin administration was associated with significant natriuretic/diuretic responses and did not influence the pressor effect and renal actions of big ET-1. (ahajournals.org)
  • 7 17 18 19 The highest concentrations of immunoreactive ET-1 in the body have been detected in the renal medulla. (ahajournals.org)
  • American Journal of Physiology - Renal Physiology Published 1 November 2017 Vol. no. (physiology.org)
  • Endothelin type B receptors (ETB-R) can induce vasodilation of the renal vasculature and also regulate tubular sodium handling. (physiology.org)
  • These data demonstrate that ET-1 synthesis is increased in renal microvessels when NO production is suppressed. (ovid.com)
  • Expression of prepro-endothelin-1 (ppET-1) mRNA was determined by quantitative real time PCR. (nih.gov)
  • The muscarinic agonist oxotremorine induced, in a tiotropium-sensitive manner, a three-fold increase in ppET-1 mRNA. (nih.gov)
  • Transforming growth factor-β(1) (TGF-β, 0.3 and 1 ng/ml) induced a three- and eight-fold increase in pp-ET-1 mRNA, respectively. (nih.gov)
  • ET-1 mRNA was analyzed by reverse transcriptase-polymerase chain reaction (RT-PCR) technique. (hindawi.com)
  • We used immunohistochemistry and in situ hybridization to detect the presence, distribution, and phenotype of ET-1-positive cells and prepro-ET-1 (pp-ET-1) mRNA-expressing cells. (physiology.org)
  • ET-1-positive stromal cells and pp-ET-1 mRNA-expressing cells were detected with different distributions and relative frequencies in normal control appendix, histologically normal appendix, and inflamed appendix. (physiology.org)
  • Six of 20 histologically normal appendixes from patients with a clinical diagnosis of acute appendicitis had many ET-1-positive stromal cells and high pp-ET-1 mRNA expression, similar to inflamed appendix. (physiology.org)
  • Forty percent of the pp-ET-1 mRNA-expressing cells were neutrophils, and the other positive cells were mast cells and macrophages. (physiology.org)
  • In this study, we investigated the presence, distribution, and phenotype of ET-1 + cells and prepro-ET-1 (pp-ET-1) mRNA-expressing cells in human appendixes, using immunohistochemistry (IHC) and a nonradioactive in situ hybridization (ISH) method, respectively. (physiology.org)
  • In this experiment lung ET-1 mRNA levels and lung mRNA expression for the ET(A) receptors were determined in lung tissue weekly (term = 42 days, intervals = 7 days). (magiran.com)
  • ET-1 treatment of cardiomyocytes increased constitutive NO synthase activity and induced NO production via the stimulation of ET-receptor subtype ET B . Using Northern blot analysis and chloramphenicol acetyltransferase assay, we found that NO suppressed the ET-1-induced increase in c- fos mRNA level and promoter activity. (aspetjournals.org)
  • Endothelin 1 is one of three isoforms of human endothelin. (wikipedia.org)
  • Three isoforms are known, each containing 21 amino acids: endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin-3 (ET-3). (clontech.com)
  • Since muscarinic up-regulation of ET-1 contributes to pro-fibrotic effects of muscarinic stimuli, inhibition of ET-1 expression could contribute to long-term beneficial effects of long-acting β(2)-adrenoceptor agonists and long-acting muscarinic antagonists. (nih.gov)
  • Experimental and preclinical studies have shown that overexpression of ET-1 axis occurs in a variety of malignancies and that ET-1 selective receptor antagonists could represent potential antitumor agents ( 11 , 12 ). (aacrjournals.org)
  • Zurück zum Zitat Ergul A. Endothelin-1 and endothelin receptor antagonists as potential cardiovascular therapeutic agents. (springermedizin.at)
  • 1 Department of Pharmacology and Cell Biophysics, University of Cincinnati College of Medicine, Cincinnati, OH 45267, USA. (nih.gov)
  • European Journal of Pharmacology , 720 (1-3), 303-309. (eur.nl)
  • Does endothelin-1 play a role in the pathogenesis of cerebral vasospasm? (biomedsearch.com)
  • SUMMARY OF REVIEW: It is generally accepted that endothelin-1 may contribute to the pathogenesis of a number of cardiovascular diseases. (biomedsearch.com)
  • ET-1 may be important in the pathogenesis of RP, and measurement of its plasma concentrations may also contribute to additional insights into the retinal hemodynamics of RP. (dovepress.com)
  • Studies of these mechanical and vasogenic factors in the pathogenesis of glaucoma have turned attention to endothelin (ET) and nitric oxide (NO), two of the main cellular mediators involved in the regulation of IOP and local ocular blood flow. (molvis.org)
  • The purpose of this study is to assess whether Naf will reduce ET-1 binding in the rabbit detrusor muscle and to assess whether there is inhibition of ET-1-mediated detrusor contraction. (clinsci.org)
  • Overall inhibition of [ 125 I]ET-1 binding by Naf was assessed using autoradiography. (clinsci.org)
  • Inhibition by nickel of endothelin-1-induced tension and associated 45Ca movements in rabbit aorta. (aspetjournals.org)
  • Preincubation of PC12 cells with pertussis toxin reversed the ET-1-induced inhibition of the K + -evoked ATP release. (aspetjournals.org)
  • Inhibition of NO synthase (NOS) or PKC abolished the ET-1 effects. (aspetjournals.org)
  • 1,2 CyA has also been implicated in the development of endothelial dysfunction and transplant vasculopathy (TxV). (ahajournals.org)
  • The aims of this study were to examine the expression level of SCUBE2 in T2DM patients with dyslipidemia and its correlation with endothelial dysfunction marker, endothelin-1 (ET-1) in this group. (bioportfolio.com)
  • Endothelin-1 secretion by alveolar macrophages in systemic sclerosis," American Journal of Respiratory and Critical Care Medicine , vol. 156, no. 5, pp. 1429-1435, 1997. (hindawi.com)
  • ab2786 labelling Endothelin 1 (green) in the secretion of HeLa cells (right) compared with a negative control (left) by Immunocytochemistry/Immunofluorescence. (abcam.com)
  • The mitogenic activity of endothelin and its ability to stimulate PtdIns(4,5)P2 and phosphatidylcholine turnover in Rat-1 fibroblasts was studied. (biochemj.org)
  • Slightly lower endothelin plasma levels were observed in patients with optic disc hemorrhages in the NTG group (p = 0.05). (molvis.org)
  • Systemic administration of Big-ET-1 triggered pressor responses and increased blood levels of immunoreactive (IR) ET-1 (1-31) and ET-1 that were reduced by more than 50% in mMCP-4 knockout (-/-) mice compared with WT controls. (sigmaaldrich.com)
  • Our results suggest that unlike the pulmonary vasculature, the guinea-pig kidney responds to ET-1 by a direct constriction, which is modulated by nitric oxide but not eicosanoids (supported by the MRCC). (lww.com)
  • In the cerebral vasculature, endothelin-1 has been proposed as a key mediator of cerebral vasospasm following subarachnoid hemorrhage. (biomedsearch.com)
  • Immunohistochemical staining of ET-1 in human corpus cavernosum tissue with this antibody results in staining of endothelial cells. (abcam.com)
  • Studies suggest that this antibody binds to an epitope in the region of ET-1 represented by amino acids 8-16. (abcam.com)
  • The anti-ECE-1 antibody was costained with anti-GFAP antibody in the whole-mount retinas. (arvojournals.org)
  • Part of the contractile response to ET-1 was inhibited by Ni2+ (0.5 mmol/L) and by a TRPC1 blocking antibody. (lu.se)
  • In the basilar artery, exhibiting less store-operated channel activity than the caudal artery, ET-1-induced contractions were insensitive to the TRPC1 blocking antibody and to mßcd. (lu.se)
  • L. Guembe and A. C. Villaro, "Immunohistochemical mapping of endothelin in the developing and adult mouse lung," Journal of Histochemistry and Cytochemistry , vol. 49, no. 10, pp. 1301-1309, 2001. (hindawi.com)
  • CONCLUSIONS: This brief review is focused on the controversial results reported by different groups concerning the possible role of endothelin-1 in narrowing of cerebral arteries exposed to autologous blood. (biomedsearch.com)
  • Black currant anthocyanins caused a normalization of serum levels of ET-1 and may slow down glaucoma progression. (greenmedinfo.com)
  • The higher ET-1-LI levels found in the FF from women undergoing gonadotropin treatment suggest a modulation by gonadotropins and/or ovarian steroids of ET-1 production by GC. (nih.gov)
  • This role of endothelin-1 is unrelated to its plasma levels. (ahajournals.org)
  • We aimed to determine the association between serial ET-1 levels and acute heart failure patient outcomes. (nih.gov)
  • Surprisingly however, these tissue levels were lower in the lungs of obese than in those of lean animals ( Figure 1A ) having similar endothelin-1 contents in the lungs as reported 5 . (nature.com)
  • Such an up-regulation of the ET B -receptor pathway in the lungs, a tissue of high endothelial cell content, would support the decreased pulmonary tissue endothelin-1 levels observed in obese mice as a likely consequence of an accelerated clearance 6 . (nature.com)
  • ET-1 plasma levels were also measured. (ahajournals.org)
  • Only SRL treatment reduced ET-1 plasma levels. (ahajournals.org)
  • Most investigators have found an increase in ET-1 levels after CyA treatment, although this is not a consistent finding. (ahajournals.org)
  • Circulating endothelin-1 (ET-1) levels are increased in cirrhosis. (portlandpress.com)
  • This relates to the severity of cirrhosis and may contribute to the increase in circulating ET-1 levels. (portlandpress.com)
  • Infusion of ET-1 caused a rise in mean arterial pressure and a fall in heart rate, and infusion of MgSO 4 returned mean arterial pressure to control levels with no effect on heart rate. (wiley.com)
  • Thus, GSK-3β appears to control the progression of wound healing and fibrosis by modulating ET-1 levels. (jci.org)
  • There are reports in the literature correlating plasma levels of ET-1 and its impact on retrobulbar hemodynamics. (dovepress.com)
  • This study evaluates aqueous humor levels of ET-1 and retrobulbar hemodynamics in patients with exfoliation syndrome (XFS) and exfoliation glaucoma (XFG). (dovepress.com)
  • All four hemodynamic parameters affected by group status significantly correlated with ET-1 levels in eyes with XFS. (dovepress.com)
  • In eyes with XFG, two of the four hemodynamic parameters significantly correlated with ET-1 levels. (dovepress.com)
  • ET-1 aqueous levels in eyes with XFG were significantly higher than those of age-matched controls. (dovepress.com)
  • ET-1 levels in eyes with XFG/XFS exhibit a significant correlation with hemodynamic parameters that indicate reduced perfusion. (dovepress.com)
  • Plasma ET-1 levels and ophthalmic features in 50 RP patients were compared with those in 20 healthy-eye control subjects. (dovepress.com)
  • Not only are both circulating and tissue levels of endothelin-1 increased in patients with atherosclerosis, but the effects of endothelin-1 are enhanced in pathophysiologic states [1]. (annals.org)
  • The aim of this study is to determining of the effects of Eicosapentaenoic acid (EPA) supplementation on serum activities of Paraoxonase-1 and Homocystein thiolactonase, and serum levels o. (bioportfolio.com)
  • Finally, pulmonary endogenous levels of IR-ET-1 were reduced by more than 40% in tissues derived from mMCP-4(-/-) mice compared with WT mice. (sigmaaldrich.com)
  • Plasma nitric oxide and endothelin-1 levels were measured at baseline and after 6 months of ERT. (annals.org)
  • Several markers such as alkaline phosphtase, 1 creatinine phosphokinase, 2 and lactate dehydrogenase 3 and procalcitonin (Pct) serum levels have been proposed for the early diagnosis of intestinal ischaemia. (pubmedcentralcanada.ca)
  • Plasma levels of endothelin 1 (ET1) have been recently associated with cardiac ischaemia. (pubmedcentralcanada.ca)
  • MMP-1, MMP-13 and NO levels were then measured by ELISA and Griess reaction, respectively. (umontreal.ca)
  • LY83583 decreased the production of both metalloproteases below basal levels, whereas the inhibitor of p38 kinase, SB202190, suppressed ET-1-stimulated production only. (umontreal.ca)
  • The Influence of Clinical and Anthropometric Parameters on the Serum Levels of the Endothelin-1 in Pregnant Women and. (srce.hr)
  • Therefore it is important to elucidate maternal and neonatal factors which influence endothelin-1 serum levels. (srce.hr)
  • In maternal blood ET-1 levels were strongly predicted by diagnosis, therapy and BMI, while umbilical cord ET-1 levels were strongly predicted by gestational age, therapy and delivery termination. (srce.hr)
  • Positive correlation between BMI and ET-1 levels suggest that obese pregnant women have increased risk for cardiovascular diseases. (srce.hr)
  • 0.42 pmol/L) big ET-1 groups according to the median value of plasma big ET-1 levels. (onmedica.com)
  • Real-time intracellular calcium level recordings were performed on PC-12 cell suspensions, and ET-1 induced a dose-dependent decrease in the K + -evoked calcium levels. (aspetjournals.org)
  • Endothelin levels were compared with genotype and allele distributions, patients' clinical status, and various risk factors for NTG. (molvis.org)
  • Plasma endothelin levels showed a noticeably positive correlation with age in the NTG group (R = 0.249, p = 0.042). (molvis.org)
  • Higher endothelin levels corresponded to more advanced visual field damage. (molvis.org)
  • No significant differences were observed regarding the endothelin levels and the frequency of notches, peripapillary atrophy, low blood pressure, cold extremities, or migraine in the two groups studied. (molvis.org)
  • There was no association between the plasma endothelin levels and the risk factors for NTG. (molvis.org)
  • In OPCAB group, ET-1 levels did not significantly vary between time points. (springermedizin.at)
  • Elevated coronary ET-1 levels after CPB in CABG group correlate with troponin-I levels 24 h postoperatively. (springermedizin.at)
  • 4,6 In addition to these pathways, common among different cell types, ET-1 stimulation results in an increase in intracellular calcium levels. (ahajournals.org)
  • Also, in five patients peripheral endothelin-1 levels were measured one and seven days after angioplasty for stenosed internal jugular veins. (termedia.pl)
  • In all collected samples thiobarbituric reacting substances were evaluated, using the spectrophotometric technique, IL1 TNF and IL6 serum levels by ELISA and endothelin 1 plasma levels by radioimmunoassay. (minervamedica.it)
  • The concentration-response curve showed a significant attenuation of endothelin-1-induced contraction in circular segments of the human superficial temporal artery. (lu.se)
  • Endothelin ETB receptor antisense or mismatch oligodeoxynucleotides showed no alteration of the endothelin-1-induced contraction. (lu.se)
  • The specific method of using the receptor antisense oligodeoxynucleotides approach revealed the presence of endothelin ETA receptors mediating contraction in the human superficial temporal artery. (lu.se)
  • Endothelin-1 (ET-1) causes urinary bladder smooth muscle contraction and the endothelin receptors A and B (ET A and ET B ) are both known to be present in the rabbit urinary bladder. (clinsci.org)
  • 0.04), e.g. at 10 -10 M ET-1, contraction was completely abolished by Naf. (clinsci.org)
  • Increased store-operated channel activity in basilar arteries after organ culture correlated with increased sensitivity of ET-1 contraction to mßcd. (lu.se)
  • Long-lasting contraction (remaining after washing away the agonist) was observed for ET-1 in RMA, but not HCMA. (eur.nl)
  • Endothelial cells convert preproendothelin to proendothelin and subsequently to mature endothelin, which the cells release. (wikipedia.org)
  • However, these enzymes cannot produce sufficient mature endothelin at the locations crucial for normal embryonic development. (biologists.org)
  • Cardiac hypertrophy induced a significant downregulation of AT 1 receptors on fibroblasts, whereas total binding and [Ca 2+ ] i sensitivity to Ang II were significantly enhanced in hypertrophied cardiomyocytes. (ahajournals.org)
  • Taken together, our findings provide the molecular basis of NO as a negative regulator in ET-1-induced cardiac hypertrophy. (aspetjournals.org)
  • Taken together, these results suggest that big ET-1-induced diuretic and natriuretic responses are mediated mainly by stimulation of nitric oxide production coupled to ET B receptor subtype activation. (ahajournals.org)
  • On the other hand, stimulation of cardiac myocytes with ET-1 causes nuclear translocation of NFATc1, which interacts with p300 and increases DNA binding. (ahajournals.org)
  • In contrast, ET-1 stimulation of c- fos expression was augmented by depletion of endogenous NO generation with the addition of NO scavenger PTIO into cardiomyocytes. (aspetjournals.org)
  • We evaluated ET-1 kinetics in cirrhosis to determine if a reduced liver clearance contributes to this process. (portlandpress.com)
  • ET-1 axis, in fact, contributes to cancer progression by several mechanisms including mitogenesis, cell survival, invasiveness, and angiogenesis ( 13 - 15 ). (aacrjournals.org)
  • Lactoferrin-endothelin-1 axis contributes to the development and invasiveness of triple-negative breast cancer phenotypes. (ptglab.com)
  • 1. Magnesium sulphate (MgSO 4 ) has been used for many years in the prevention of eclamptic seizures, but its mechanism of action has never been elucidated. (clinsci.org)
  • The infusion of ET-1 (0.5 and 1 μM, 5 min) in the guinea-pig kidney did not induce the release of prostacyclin or thromboxane. (lww.com)
  • More precisely, ET-1 3 4 5 6 and Ang II 3 7 induce the hypertrophic phenotype in cultured cardiomyocytes. (ahajournals.org)
  • The extra stimuli that induce hypertrophy include mechanical overload and neurohumoral factors such as endothelin-1 (ET-1). (aspetjournals.org)
  • Hyperbaric oxygenation in healthy volunteers can induce not only lipid peroxidation, but also liberation of compounds such as TNFα and endothelins, no matter whether pure oxygen is breathed or not. (minervamedica.it)
  • C. L. Golden, J. P. Kohler, H. S. Nick, and G. A. Visner, "Effects of vasoactive and inflammatory mediators on endothelin-1 expression in pulmonary endothelial cells," American Journal of Respiratory Cell and Molecular Biology , vol. 12, no. 5, pp. 503-512, 1995. (hindawi.com)
  • This mini-review surveys epidemiological and experimental air pollution studies focused on ET-1 dysregulation as a plausible mechanism underlying the development of cardiovascular disease. (springer.com)
  • The central administration of endothelins modulates endocrine and cardiovascular regulation and behavior ( van den Buuse, 1997 ). (frontiersin.org)
  • In spite of a chronically reduced ADC, typically associated with ischaemia-induced energy failure, a 31 P MRS-detectable reduction in the phosphocreatine (PCr) to gamma adenosine triphosphate (γATP) ratio was not observed at any time point in either age group, suggesting dissociation of tissue water diffusion and metabolic changes within the ET-1-induced lesion. (springer.com)
  • The aim of this study was to investigate whether the previously reported anti-arrhythmic effect of endothelin-1 (ET-1) is mediated by degranulation of cardiac mast cells prior to myocardial ischaemia. (strath.ac.uk)
  • A parallel series of sham groups were performed to determine the direct effects of ET-1 and compound 48/80 on mast cell degranulation in the absence of ischaemia. (strath.ac.uk)
  • These results demonstrate for the first time that when given prior to ischaemia ET-1 mediates its anti-arrhythmic effects, at least in part, via cardiac mast cell degranulation. (strath.ac.uk)
  • Here, the effects of a single intravitreal (IVT) injection of TA were compared with those of NCX 434 on intraocular pressure (IOP), retinal function and retrobulbar haemodymamics in endothelin-1 (ET-1) induced ONH ischaemia/reperfusion in rabbits. (bmj.com)
  • Conclusion NCX 434 attenuates ET-1 induced ischaemia/reperfusion damage without increasing IOP, probably due to NO release. (bmj.com)
  • In this study, we investigate NO modulation of cellular signaling in endothelin-1 (ET-1)-induced cardiomyocyte hypertrophy in culture. (aspetjournals.org)
  • Therefore, the purpose of this study was to examine the effect of ET-1 on NO production and elucidate how NO is involved in ET-1-induced cardiomyocyte hypertrophy. (aspetjournals.org)
  • In addition to the systemic circulation, endothelin production and endothelin receptors have been demonstrated in the central nervous system. (frontiersin.org)
  • These results suggest that targeting the GSK-3β pathway or ET-1 may be of benefit in controlling tissue repair and fibrogenic responses in vivo. (jci.org)
  • NCX 434 attenuated ET-1 induced oxidative stress markers and nitrotyrosine in retinal tissue, and interleukin-6 and tumour necrosis factor-α in aqueous humour more effectively than TA. (bmj.com)
  • The aim of this study was the assessment of the level of endothelin-1 (ET-1), tumor necrosis factor (TNF-α), interleukin-6 (IL-6), soluble IL-6 receptor (IL-6sR), von Willebrand's factor (vWF) and platelet factor 4 (PF-4) in patients with Raynaud's phenomenon associated with systemic connective tissue diseases. (minervamedica.it)
  • In this study, the endothelin-1 (ET-1) and nitric oxide (NO) concentrations in slow coronary flow (SCF) patients were assessed before and at the peak of the exercise stress test and compared with the values from healthy controls. (go.jp)
  • 20 mg·kg−1·h−1) prior to coronary artery occlusion (CAO). (strath.ac.uk)
  • Increased mortality with elevated plasma endothelin-1 in acute heart failure: an ASCEND-HF biomarker substudy. (nih.gov)
  • We measured plasma ET-1 at baseline, 48-72 h, and 30 days in a cohort of 872 patients hospitalized with acute heart failure from the ASCEND-HF trial (randomized to nesiritide vs. placebo), and its association with 30-day mortality, 180-day mortality, in-hospital death or worsening heart failure, and 30-day mortality or rehospitalization. (nih.gov)
  • We observed an independent association between elevated ET-1 and short-term in-hospital clinical outcomes and 180-day mortality in hospitalized patients with acute heart failure ET-1 provided additional prognostic information which was incremental to that yielded by NT-proBNP. (nih.gov)
  • Furthermore, extensive acute T 1 -w hypointensity was observed in the presence of cytotoxic oedema-induced T 2 -w changes, whereas other authors have shown that increased T 1 values following MCAO reflect vasogenic oedema. (springer.com)
  • In contrast, the selective ETB-receptor agonist, IRL-1620 (1-1000 pmol) was found to be inactive. (lww.com)
  • Moreover, further research may test the efficacy of selective ET-1 pharmacological interventions (e.g. (springer.com)
  • Type 1 Diabetes Mellitus (T1DM) is a well-studied autoimmune disease resulting in insulin deficiency due to selective β-cell destruction. (bioportfolio.com)
  • For this purpose we measured endothelin-1 concentrations in blood samples that were obtained during selective catheterisation of the main veins draining the central nervous system: the internal jugular veins and the azygous vein. (termedia.pl)
  • Soluble fractions from the lungs, left cardiac ventricle, aorta, and kidneys of WT but not mMCP-4(-/-) mice generated ET-1 (1-31) from exogenous Big-ET-1 in a TY-51469-sensitive fashion as detected by high-performance liquid chromatography/ matrix-assisted laser desorption/ionization-mass spectrometry. (sigmaaldrich.com)
  • 5 Potential mechanisms resulting in vasospasm include the increased release of vasoconstrictors such as endothelin-1 (ET-1) or increased sensitivity to these vasoconstrictors. (ahajournals.org)
  • The aim of this study was to elucidate the role of endothelin-1 (ET-1) in the pathophysiology of retinitis pigmentosa (RP). (dovepress.com)
  • The results of this study show that endothelial function (assessed by ET-1 and NO concentrations) and its response to exercise were abnormal in SCF patients compared with healthy subjects, and this may play some pathophysiologic role. (go.jp)
  • Endothelin-1 (ET-1) axis plays a crucial role in angiogenesis and tumorigenesis. (aacrjournals.org)
  • To investigate the role of endothelin-1 (ET-1) in retinal glial cells in regulating retinal blood flow (RBF) during hyperoxia in cats. (arvojournals.org)
  • The current findings suggest that retinal glial ET-1 may play an important role in regulating RBF during hyperoxia in cats. (arvojournals.org)
  • Pivotal role of mouse mast cell protease 4 in the conversion and pressor properties of Big-endothelin-1. (sigmaaldrich.com)
  • Our results show that mMCP-4 plays a pivotal role in the dynamic conversion of systemic Big-ET-1 to ET-1 in the mouse model. (sigmaaldrich.com)
  • Plasma and cardiac ET-1 concentrations and ET-1 receptor regulation on both ventricular cell types are not altered in cardiac volume overload, suggesting that cardiac ET-1 may not play a significant role in this model. (ahajournals.org)
  • To determine the prognostic role of big endothelin-1 (ET-1) in left ventricular non-compaction cardiomyopathy (LVNC).We prospectively enrolled patients whose LVNC was diagnosed by cardiac MRI and who had big ET-1 data available. (onmedica.com)
  • In another context, several studies have reported that endothelin-1 and its receptor ETAR also play a central role in the development of tumour cell invasion and metastasis. (bmj.com)
  • 1 Among the various mediators implicated in this putatively stretch-induced smooth muscle cell (SMC) hyperplasia, endothelin-1 (ET-1) may play a pivotal role. (ahajournals.org)
  • These findings prompted us to investigate the role of NFATc in ET-1-dependent and p300-dependent bcl-2 transcription in cardiac myocytes. (ahajournals.org)