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.
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.
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.
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
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)

TY - JOUR. T1 - Weight loss reduces plasma endothelin-1 concentration in obese men. AU - Maeda, Seiji. AU - Jesmin, Subrina. AU - Iemitsu, Motoyuki. AU - Otsuki, Takeshi. AU - Matsuo, Tomoaki. AU - Ohkawara, Kazunori. AU - Nakata, Yoshio. AU - Tanaka, Kiyoji. AU - Goto, Katsutoshi. AU - Miyauchi, Takashi. PY - 2006/6. Y1 - 2006/6. N2 - Obesity is associated with endothelial dysfunction that may contribute to the development of diabetes, hypertension, and atherosclerosis. Endothelin-1 (ET-1), which is produced mostly by vascular endothelial cells, has potent vasoconstrictor and proliferative activity in vascular smooth muscle cells and, therefore, has been implicated in regulation of vascular tonus and the progression of atherosclerosis, suggesting that ET-1 may be important in endothelial dysfunction. We studied whether diet-induced weight loss (i.e., lifestyle modification) affects plasma ET-1 concentration in obese individuals. We measured plasma ET-1 concentration in seven obese men (age: 48 ...
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.
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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 ...
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
This article shows how to create a Windows Presentation Foundation (WPF) application from scratch (an empty project) and do it with a program that has a Main function.
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... (ET-1), also known as preproendothelin-1 (PPET1), is a potent vasoconstrictor peptide produced by vascular ... Endothelin-1 receptor antagonists (Bosentan) are used in the treatment of pulmonary hypertension. Use of these antagonists ... Overview of all the structural information available in the PDB for UniProt: P05305 (Endothelin-1) at the PDBe-KB. This article ... The protein encoded by this gene - EDN1 - is proteolytically processed to release endothelin 1. Endothelin 1 is one of three ...
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) Portal: Biology v t e (EC ... Endothelin-converting enzyme 1 (EC, 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 ...
2003). "Shear stress attenuates endothelin and endothelin-converting enzyme expression through oxidative stress". Regul. Pept. ... Endothelin converting enzyme 1, also known as ECE1, is an enzyme which in humans is encoded by the ECE1 gene. Endothelin- ... "Entrez Gene: ECE1 endothelin converting enzyme 1". Schmidt M, Kröger B, Jacob E, Seulberger H, Subkowski T, Otter R, Meyer T, ... 1996). "Human endothelin converting enzyme gene (ECE1) mapped to chromosomal region 1p36.1". Cytogenet. Cell Genet. 72 (4): 322 ...
Endothelin receptor type B, also known as ETB is a protein that in humans is encoded by the EDNRB gene. Endothelin receptor ... "Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and enteric ... "Entrez Gene: EDNRB endothelin receptor type B". Sato-Jin K, Nishimura EK, Akasaka E, Huber W, Nakano H, Miller A, Du J, Wu M, ... Its ligand, endothelin, consists of a family of three potent vasoactive peptides: ET1, ET2, and ET3. A splice variant, named ...
Endothelin receptor type A, also known as ETA, is a human G protein-coupled receptor. Endothelin receptor type A has been shown ... "Entrez Gene: EDNRA endothelin receptor type A". Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the ... Lee HJ, Chun M, Kandror KV (May 2001). "Tip60 and HDAC7 interact with the endothelin receptor a and may be involved in ... "Endothelin Receptors: ETA". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ...
1995). "Interaction of endothelin-3 with endothelin-B receptor is essential for development of epidermal melanocytes and ... The active peptide is a ligand for endothelin receptor type B (EDNRB). The interaction of this endothelin with EDNRB is ... The protein encoded by this gene is a member of the endothelin family. Endothelins are endothelium-derived vasoactive peptides ... 1990). "One of the endothelin gene family, endothelin 3 gene, is expressed in the placenta". FEBS Lett. 261 (2): 327-30. doi: ...
Barnes K, Turner AJ; Turner (August 1997). "The endothelin system and endothelin-converting enzyme in the brain: molecular and ... 2016) 'Endothelin' Pharmacol. Rev. 68: 357-418. pmid =26956245 doi =10.1124/pr.115.011833 "Endothelin Receptors". IUPHAR ... Endothelin+receptor at the US National Library of Medicine Medical Subject Headings (MeSH) v t e (Articles with short ... There are at least four known endothelin receptors, ETA, ETB1, ETB2 and ETC, all of which are G protein-coupled receptors whose ...
The association between endothelins, poor prognosis and invasion suggests the endothelin axis is an interesting therapeutic ... ET-2 acts by binding to two different G-protein coupled receptors (GCPRs), the endothelin A receptor (EDNRA) and the endothelin ... As a strong positive inotrope, endothelin-2 has an impact on the human myocardium and for this reason, endothelin-2 antagonists ... endothelin-2 and endothelin-receptor-A genotyped by four duplex assays and seven simple assays on a LightCycler using ...
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 ...
Ariza AC, Bobadilla NA, Halhali A (2007). "[Endothelin 1 and angiotensin II in preeeclampsia]". Revista de Investigacion ... 183 (1): 8-13. doi:10.1016/0006-291X(92)91600-U. PMID 1543512. Takayanagi R, Ohnaka K, Sakai Y, Nakao R, Yanase T, Haji M, et ... 5 (1): 45-61. doi:10.1210/edrv-5-1-45. PMID 6368215. Marvar PJ, Goodman J, Fuchs S, Choi DC, Banerjee S, Ressler KJ (June 2014 ... 47 (1): 17-28. doi:10.1016/S0361-9230(98)00039-2. PMID 9766385. S2CID 24936475. Berry C, Touyz R, Dominiczak AF, Webb RC, Johns ...
"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 ...
Yamaguchi T, Murata Y, Fujiyoshi Y, Doi T (April 2003). "Regulated interaction of endothelin B receptor with caveolin-1". ... endothelin receptor type B, PDGFRB, PDGFRA, PTGS2, TRAF2, estrogen receptor alpha, caveolin 2, PLD2, Bruton's tyrosine kinase, ... Caveolin-1 is a protein that in humans is encoded by the CAV1 gene. The scaffolding protein encoded by this gene is the main ... Caveolin 1 has been shown to interact with heterotrimeric G proteins, Src tyrosine kinases (Src, Lyn) and H-Ras,cholesterol,TGF ...
Endothelins are peptides with receptors and effects in many body organs. Endothelin constricts blood vessels and raises blood ... Endothelins are the most potent vasoconstrictors known. Overproduction of endothelin in the lungs may cause pulmonary ... endothelin-2 (ET-2), and endothelin-3 (ET-3) are located on chromosomes 6, 1, and 20, respectively. Endothelin functions ... Endothelins at the US National Library of Medicine Medical Subject Headings (MeSH) (Protein pages needing a picture, Genes on ...
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. Bibcode:2004Natur.432.. ... 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- ...
... (INN, trade name Pivlaz) is a drug belonging to the class of endothelin receptor antagonists. The endothelin 1 ... Endothelin receptor antagonists, Vasodilators, Tetrazoles, Pyridines, Sulfonamides, Pyrimidines, Methoxy compounds, Diaryl ...
... , which relaxes those muscles, is an endothelin receptor antagonist, and is selective for the type A endothelin ... Endothelin binds to two receptors, ETA and ETB. ETA is responsible for cell growth in the vessels as well as vasoconstriction, ... 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 ...
Martins et al., 2016 find blockade of endothelin-1 prevents CMM and its symptoms and supplementation helps to produce it. ... Martins et al., 2016 find endothelin-1 production is vital to CMM disease progression. Subramaniam et al., 2015 find mice ... Martins et al., 2016 find NK65 can produce CMM under supplementation of endothelin-1. See section above for specific molecules ... 575 Endothelin 1 has an uncertain role in producing cerebral murine malaria. ...
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 ... Jones, TA (1 April 1994). "Use-Dependent Growth Of Pyramidal Neurons After Neocortical Damage". The Journal of Neuroscience. 14 ... Theresa Jones was born in Pine Bluff, Arkansas on November 1, 1964. Throughout her childhood, her family moved around to Little ... 1): 156-160 May 22, 1992 Times Cited: 148 Jones TA, Chu Cj, Grande La, Et Al. "Motor Skills Training Enhances Lesion-Induced ...
The pathogenesis of cerebral vasospasm following subarachnoid hemorrhage is attributed to the higher levels of endothelin 1, a ... 2007). "Novel mechanism of endothelin-1-induced vasospasm after subarachnoid hemorrhage". Journal of Cerebral Blood Flow & ... Oxyhaemoglobin in cerebrospinal fluid (CSF) causes vasoconstriction by increasing free radicals, endothelin-1, prostaglandin ... which increases and decreases the production of endothelin 1 and endothelial NOS, respectively, the issue that yields in ...
... 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, a few ... The main differences in the family of endothelin and sarafotoxins appear at N-terminal of peptides, as C-terminal in all of ...
March 2021). "Endothelin-1 drives invadopodia and interaction with mesothelial cells through ILK". Cell Reports. 34 (9): 108800 ... 97 (1): 185-9. Bibcode:2000PNAS...97..185M. doi:10.1073/pnas.97.1.185. PMC 26637. PMID 10618392. Soutoglou E, Papafotiou G, ... 89 (1-2): 18-23. doi:10.1159/000015583. PMID 10894930. S2CID 22901214. de Curtis I (September 2019). "The Rac3 GTPase in ... 89 (1-2): 18-23. doi:10.1159/000015583. PMID 10894930. S2CID 22901214. Gnanapragasam VJ, Leung HY, Pulimood AS, Neal DE, Robson ...
Fernandez-Patron, C., Radomski, M. W., & Davidge, S. T. (1999). Vascular matrix metalloproteinase-2 cleaves big endothelin-1 ... Hypertension, 33(1), 83-89. Roggensack, A. M., Zhang, Y., & Davidge, S. T. (1999). Evidence for peroxynitrite formation in the ... Hypertension, 33(1), 83-89. "Sandra T Davidge, PhD, FRSC, FCAHS - [email protected]". apps.ualberta.ca. Retrieved 2022-04-03. ... Tier 1) in Maternal and Perinatal Cardiovascular Health for two terms, and was the President of the Society for Reproductive ...
Various vasoactive agents, such as prostanoids, phosphodiesterase inhibitors, and endothelin antagonists, are approved for the ... Important vasoactive substances are angiotensin-11, endothelin-1, and alpha-adrenergic agonists. ...
... endothelin receptor, endothelin converting enzyme, breast cancer regression proteins and matrix metanosomal proteins as well as ... 1]. Before going for his bachelor's degree in Science in Allahabad University, Tej Pal Singh has studied in his neighbourhood ... 529 (1): 1-10. doi:10.1016/j.abb.2012.11.001. ISSN 1096-0384. PMID 23149273. Singh, Avinash; Kumar, Ashok; Gautam, Lovely; ... 8 (1): e53756. Bibcode:2013PLoSO...853756S. doi:10.1371/journal.pone.0053756. ISSN 1932-6203. PMC 3541179. PMID 23326499. Singh ...
"Atrial natriuretic peptides negatively and positively modulate circulating endothelin in humans". Metabolism. 45 (3): 315-9. ... 2011: 1-13. doi:10.1155/2011/835671. PMC 3144715. PMID 21808648. Chen Y, Zhuang J, Zhang L, Li Y, Jin Z, Zhao Z, Zhao Y, Zhou H ... 63 (1): 150-2. doi:10.1212/01.WNL.0000130250.62842.C9. PMID 15249626. Hunt WT, Zimmermann EF, Hilton MP (April 2012). " ... 63 (1): 150-2. doi:10.1212/01.WNL.0000130250.62842.C9. PMID 15249626. (Articles with short description, Short description is ...
BMPER is inhibited by endothelin-1, which may be mediated by endothelin inhibition of KLF15. GRCh38: Ensembl release 89: ...
Corticotropin-releasing hormone Sauvagine Urocortin Antagonists Astressin-B Agonists Endothelin 1 Endothelin 2 Endothelin 3 IRL ... 1-15) Galanin-like peptide Galmic Galnon NAX 810-2 Antagonists C7 Dithiepine-1,1,4,4-tetroxide Galantide (M15) M32 M35 M40 SCH- ... against IGF-1 and IGF-2) Agonists Kisspeptin (kisspeptin-54, metastin) Kisspeptin-10 KISS1-305 MVT-602 (RVT-602, TAK-448) TAK- ... 1-15) Galmic Galnon Antagonists C7 Galantide (M15) GalR3ant HT-2157 M32 M35 M40 SNAP-37889 SNAP-398299 Agonists Albiglutide ...
Chronic hemolysis may also lead to endothelial dysfunction, heightened endothelin-1-mediated responses and vasculopathy. The ... ISBN 978-1-4058-8118-0. Witek, K; Ścisłowska, J; Turowski, D; Lerczak, K; Lewandowska-Pachecka, S; Pokrywka, A (March 2017). " ... 94 (1): 38-42. doi:10.1152/japplphysiol.00631.2001. PMID 12391035. S2CID 5750453. Lippi G, Schena F, Salvagno GL, Aloe R, Banfi ... 34 (1): 45-48. doi:10.5114/biolsport.2017.63732. ISSN 0860-021X. PMC 5377560. PMID 28416897. Madigan, Michael T. (2010). Brock ...
Gonsalves C, Kalra VK (November 2010). "Endothelin-1-induced macrophage inflammatory protein-1beta expression in monocytic ... 27 (1): 250-7. doi:10.3892/or.2011.1472. PMID 21947305. Brenner B, Hoshen MB, Purim O, David MB, Ashkenazi K, Marshak G, Kundel ... cells involves hypoxia-inducible factor-1alpha and AP-1 and is negatively regulated by microRNA-195". J. Immunol. 185 (10): ...
... endothelin receptor - endothelin-1 - energy decomposition cycles - energy level - enhancer - enkephalin - enthalpy - entomology ... IGF type 1 receptor - IGF type 2 receptor - IgG - IgM - immediate-early protein - immune cell - immune system - immunoglobulin ... alpha-1 adrenergic receptor - alpha-2 adrenergic receptor - alpha-beta T-cell antigen receptor - alpha-fetoprotein - alpha- ... intercellular adhesion molecule-1 - interferon receptor - interferon type I - interferon type II - interferon-alpha - ...
3-Dicarbonyl Compounds to Nitroalkenes for the Synthesis of Endothelin-A Antagonist ABT-546. Scope, Mechanism, and Further ... "Development of a Catalytic Enantioselective Conjugate Addition of 1, ...
5 (1): 23-6. doi:10.4161/cc.5.1.2305. PMID 16357527. Kazanskaya O, Glinka A, del Barco Barrantes I, Stannek P, Niehrs C, Wu W ( ... 352 (1): 1-13. doi:10.1016/j.ydbio.2011.01.004. PMC 3089906. PMID 21237142. Cadieu E, Neff MW, Quignon P, Walsh K, Chase K, ... RSPO2 has been proposed to regulate craniofacial patterning and morphogenesis within pharyngeal arch 1 through ectoderm- ... mesenchyme signaling via the endothelin-Dlx5/6 pathway. In dogs, a variant on the Rspo2 gene is associated moustache and ...
... endothelin, and atrial natriuretic peptide. Associations have been observed between neprilysin expression and various types of ... endothelin, and atrial natriuretic peptide. Some are intended to treat heart failure. Sacubitril/valsartan (Entresto/LCZ696), ... 32 (1): 2-3. doi:10.1097/MPH.0b013e3181c74aca. PMID 20051779. Madani R, Poirier R, Wolfer DP, Welzl H, Groscurth P, Lipp HP, Lu ... 310 (1): 236-41. doi:10.1016/j.bbrc.2003.09.003. PMID 14511676. Sahli S, Stump B, Welti T, Schweizer WB, Diederich R, Blum- ...
Endothelin Okada, M; Nishikibe, M (Winter 2002). "BQ-788, a selective endothelin ET(B) receptor antagonist". Cardiovascular ... 20 (1): 53-66. doi:10.1111/j.1527-3466.2002.tb00082.x. PMID 12070534. v t e (Articles without EBI source, Articles without KEGG ...
Metallinos, DL; Bowling AT; Rine J (June 1998). "A missense mutation in the endothelin-B receptor gene is associated with ... is produced by the Ile118Lys mutation on the equine Endothelin receptor type B gene and when homozygous produces lethal white ... Sabino 1 and the other KIT alleles in horses are not known to cause blue eyes. Blue eyes are linked to splashed white genes, ... Neither Sabino 1 or any other alleles of W are linked to lethal white syndrome (LWS). LWS occurs when a foal is homozygous for ...
Endothelin converting enzyme-2. Bradykinin is a potent endothelium-dependent vasodilator and mild diuretic, which may cause a ... 93 (1): 89-92. doi:10.1016/j.jep.2004.03.030. PMID 15182910. Yagi A, Harada N, Yamada H, Iwadare S, Nishioka I (October 1982 ... 24 (1): 163-69. doi:10.1111/j.1476-5381.1965.tb02091.x. PMC 1704050. PMID 14302350. Lotz-Winter H (June 1990). "On the ... McLean PG, Ahluwalia A, Perretti M (August 2000). "Association between kinin B(1) receptor expression and leukocyte trafficking ...
... under the control of a modified version of the murine promoter for endothelin-1, which is called PPE-1. PPE-1 drives tissues ... Demos, Telis (1 October 2014). "Vascular Biogenics Revives Its U.S. IPO". Wall Street Journal. (Articles with short description ... a chimeric gene encoding a fusion protein that combines the extracellular and intramembrane domains of the human TNF receptor 1 ...
... endothelin receptor type B ELF1: encoding protein E74-like factor 1 (ets domain transcription factor) ESD: S-formylglutathione ... ISBN 978-1-136-84407-2. Genome Decoration Page, NCBI. Ideogram data for Homo sapience (850 bphs, Assembly GRCh38.p3). Last ... ISBN 978-1-4673-1921-8. S2CID 16666470. "p": Short arm; "q": Long arm. For cytogenetic banding nomenclature, see article locus ... ARGLU1: encoding protein Arginine and glutamate-rich protein 1 ATP7B: ATPase, Cu++ transporting, beta polypeptide (Wilson ...
Çuhadar, Serap; Semerci, Tuna (2016). "Renal Biomarkers N-Acetyl-Beta-d-Glucosaminidase (NAG), Endothelin, and Their ... EC 3.2.1 refers to a glycosidase: an enzyme that hydrolyses oxygen- and sulfur-glycosol compounds. EC refers to n- ... 170 (1): 63-67. doi:10.1016/0378-1119(95)00848-9. ISSN 0378-1119. PMID 8621090. VORGIAS, C. E.; PERRAKIS, A.; TEWS, I. (October ... 799 (1 Enzyme Engine): 190-192. Bibcode:1996NYASA.799..190V. doi:10.1111/j.1749-6632.1996.tb33198.x. ISSN 0077-8923. PMID ...
Similarly, the intracerebral gene transfer of ECE (endothelin-converting enzyme) via a virus vector stereotactically injected ... September 2008). "Adeno-associated viral (AAV) serotype 5 vector mediated gene delivery of endothelin-converting enzyme reduces ... 8 (1): 2. doi:10.1186/1472-6939-8-2. PMC 1851967. PMID 17394662. Alexander B, Warner-Schmidt J, Eriksson T, Tamminga C, Arango- ... 32 (1): 75-92. doi:10.13140/RG.2.2.11026.89289. "1990 The Declaration of Inuyama". 5 August 2001. Archived from the original on ...
"Endothelin-1 induces myofibrillar disarray and contractile vector variability in hypertrophic cardiomyopathy-induced ... 3010del MYBPC3 mutation that exhibited in addition to hypertrophy contractile variability in the presence of endothelin-1. ... 12 (1): 101-13. doi:10.1016/j.stem.2012.10.010. PMC 3638033. PMID 23290139. Han L, Li Y, Tchao J, Kaplan AD, Lin B, Li Y, Mich- ... 82 (1): 130-3. doi:10.1161/01.res.82.1.130. PMID 9440712. Carrier L, Bonne G, Bährend E, Yu B, Richard P, Niel F, Hainque B, ...
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- ...
A number of hormones influence arteriole tone such as angiotensin II (vasoconstrictive), endothelin (vasoconstrictive), ... ISBN 0-13-981176-1. Rahman, Masum; Abu Bakar, Siddik (4 December 2021). StatPearls [Internet] (Updated ed.). Treasure Island ( ... are vasoconstrictive acting on alpha 1-adrenergic receptors. However, the arterioles of skeletal muscle, cardiac muscle, and ...
Takahashi, Ghatei, Lam, H a l l o r a n, and B l o o m. "Elevated Plasma Endothelin in Patients with Diabetes Mellitus." ... Oxytocin (OXT) Omentin Endothelin-1 Nesfatin-1 Irisin Betatrophin Hepatocyte growth factor (HGF) Fibroblast growth factor - ... "Evaluation of Oxytocin (OXT), Endothelin-1 and Nesfatin Plasma Concentrations in Newly-diagnosed Diabetic and Non-diabetic ... "Evaluation of Oxytocin (OXT), Endothelin-1 and Nesfatin Plasma Concentrations in Newly-diagnosed Diabetic and Non-diabetic ...
NEP-like enzymes include the endothelin-converting enzymes. The peptidase M13 family believed to activate or inactivate ... 144 (1): 59-66. doi:10.1016/S0006-291X(87)80475-8. PMID 3555489. Turner AJ, Isaac RE, Coates D (March 2001). "The neprilysin ( ...
... role of endothelin-1". Am. J. Physiol. Endocrinol. Metab. 285 (2): E390-6. doi:10.1152/ajpendo.00509.2002. PMID 12721154. ... 373 (1): 23-29. doi:10.1016/0014-5793(95)01006-Z. PMID 7589426. S2CID 25033358. Usdin TB, Mezey E, Button DC, et al. (1994). " ... 63 (1): 17-22. doi:10.1016/0167-0115(96)00019-5. PMID 8795084. S2CID 42462407. N'Diaye N, Tremblay J, Hamet P, et al. (1998). " ... 1997). "GLP-1/GIP chimeric peptides define the structural requirements for specific ligand-receptor interaction of GLP-1". ...
... and endothelin receptor antagonists have no effect, and in some cases worsen of the EIPH. A non-pharmacological nasal strip, ... Blood can usually be detected in the trachea or bronchi for 1-3 days after an episode of EIPH, but may be present for up to a ... 19 (1): 87-100. doi:10.1016/S0749-0739(02)00068-8. PMID 12747663. Epp, TS; Edwards, KL; Poole, DC; Erickson, HH (17 December ... p. [page needed]. ISBN 978-0-9654461-1-2. Roberts, C.A., Hillidge, C. and Marlin, D.J. (1993) Exercise induced pulmonary ...
... for example discovering one of the mechanisms to activate endothelin and that a mutation in endothelin receptor can cause ... including working with Takeshi Sakurai to identify the receptor for endothelin. He kept studying endothelin after moving to the ... Vane, John (1990). "Endothelins come home to roost" (PDF). Nature. 348 (6303): 673. doi:10.1038/348673a0. PMID 2175394. S2CID ... Yanagisawa is most well known for his discovery of the hormone endothelin and the neuropeptide orexin. Early 1980s saw the ...
Miller, C. T. (2003). "Two endothelin 1 effectors, hand2 and bapx1, pattern ventral pharyngeal cartilage and the jaw joint". ... 4 (1): 16. doi:10.1186/s40851-018-0101-3. PMC 5998585. PMID 29942645. Rainbow RS, Heenam K, Li Z, et al. (2014). "The role of ... 266 (1): 138-150. doi:10.1016/j.ydbio.2003.10.012. PMID 14729484. Lukas, Paul; Olsson, Lennart (2018). "Bapx1 is required for ... 199 (Pt 1-2): 181-7. doi:10.1111/j.1469-7580.2008.00944.x. PMC 1594973. PMID 11523821. Hellemans, Jan; Simon, Marleen; Dheedene ...

No data available that match "endothelin 1"

  • ET-1 is a potent vasoconstrictor secreted by endothelial cells. (bmgrp.com)
  • The present study was designed to evaluate the role of endothelin (ET)-1, a potent endogenous vasoconstrictor, in the genesis of vasospasm in glaucoma. (arvojournals.org)
  • The vasoconstrictor activities of the iodinated ET-1 were confirmed to be similar to those of native ET-1. (elsevier.com)
  • Obesity is associated with endothelial dysfunction related to decreased NO bioavailability, increased endothelin 1 vasoconstrictor activity, and decreased circulating ghrelin. (unicatt.it)
  • In patients with metabolic syndrome, ghrelin has benefits to normalize the balance between vasoconstrictor (endothelin 1) and vasodilating (NO) mediators, thus suggesting that this peptide has important peripheral actions to preserve vascular homeostasis in humans. (unicatt.it)
  • Endothelins are endothelium-derived vasoconstrictor peptides. (cusabio.com)
  • Endothelin-1, more commonly known as a potent vasoconstrictor, is a normal ejaculate protein that also stimulates osteoblasts. (nsw.gov.au)
  • [7] Besides its vasoconstrictor effects ET-1 also contributes to cell proliferation, thereby promoting vascular growth and atherogenesis. (ijp-online.com)
  • The potent vasoconstrictor endothelin 1 (ET-1) is thought to arise from the proteolytic processing of big endothelin 1 (Big ET) by a unique endothelin-converting enzyme, possibly a metalloprotease. (uab.edu)
  • Twenty-four 1-d-old broilers were distributed in 2 groups, pulmonary hypertensive broilers (PHB) and pulmonary nonhypertensive broilers (NPHB), to estimate possible differences between them in the expression of endothelin 1 (ET-1) and its type A receptor, connective tissue growth factor, platelet-derived growth factor, and adrenomedullin expression in the lungs. (eurekamag.com)
  • Because endothelin-1 (ET-1), a paracrine hormone produced by vascular endothelial cells, has vasoactive properties, we investigated the hemodynamic effects of intrapulmonary injections of ET-1 in eight intact newborn lambs at rest and during pulmonary hypertension. (elsevier.com)
  • At rest, ET-1 (50-1,000 ng/kg) did not change pulmonary arterial pressure. (elsevier.com)
  • ET-1 is a pulmonary vasodilator during pulmonary hypertension in the intact newborn lamb. (elsevier.com)
  • 1 Elevated PA pressure (PAP) can be caused by abnormalities in the precapillary pulmonary arterioles, called pulmonary arterial hypertension (PAH), or by abnormalities that increase left atrial pressure resulting in back pressure on the pulmonary circulation, called pulmonary venous hypertension (PVH). (clevelandclinicmeded.com)
  • Congenital diaphragmatic hernia: endothelin-1, pulmonary hypertension, and disease severity. (medscape.com)
  • 1 , 4 WHO group 1 refers to pulmonary arterial hypertension, characterized by the progressive remodelling, narrowing and obliteration of small pulmonary arteries due to proliferation of smooth muscle and endothelial cells, vascular wall inflammation and fibrosis. (cmaj.ca)
  • Results: MCT caused increased RVP, medial wall thickening of the pulmonary arterioles, and increased expression level of ET-1, ET receptor A, and NADPH oxidase (NOX) 4 proteins. (ewha.ac.kr)
  • We confirmed that ET-1 increased NOX4 level and decreased glutathione peroxidase-1 level in pulmonary artery smooth muscle cells (PASMCs). (ewha.ac.kr)
  • Bosentan is an endothelin receptor antagonist indicated for the treatment of pulmonary arterial hypertension (PAH) in patients with WHO class III or IV symptoms. (medscape.com)
  • A new consensus survey of expert opinions was published regarding the use of oral prostacyclin pathway agents in patients with various forms of pulmonary arterial hypertension (PAH) who received dual endothelin receptor antagonist (ERA)/phosphodiesterase type 5 inhibitor (PDE5i) therapy. (pulmonologyadvisor.com)
  • Pulmonary vasodilators have historically shown mixed results in PH, and current IPF guidelines recommend against use of sildenafil or endothelin receptor agonists. (medscape.com)
  • 1. The present study evaluated changes in autonomic control of the cardiovascular system in conscious rats following blockade of endothelin (ET) receptors with bosentan. (shengsci.com)
  • abstract = "The rate of elimination and the fate of endothelin-1 (ET-1) from the circulating blood was studied in urethane-anesthetized rats by intravenous injection of [125I]-labeled ET-1. (elsevier.com)
  • High levels of ET-1 and its receptors are expressed in both endothelial cells and circulating in the blood of SSc patients. (degruyter.com)
  • Endothelin system was first purified and sequenced in the late 1980s from cultured endothelial cells [ 1 ]. (degruyter.com)
  • [3] Atherosclerosis is a progressive and systemic vascular disorder that initiates molecular and cellular events that are triggered by endothelial dysfunction, resulting in decreased nitric oxide production, increased ET-1 production and cyclooxgenase activity, and inflammation. (ijp-online.com)
  • The 21-amino acid peptide endothelin-1 (ET-1) is produced by vascular endothelial cells from the 38-amino acid precursor peptide, big ET-1, by the action of endothelin converting enzyme (ECE). (ijp-online.com)
  • To explore the role of endothelin-1 (ET-1) and leptin in intrauterine growth restriction (IUGR) among preeclamptic and non-pre-eclamptic women. (who.int)
  • The crystal structure of human endothelin. (nih.gov)
  • Solubilization and characterization of endothelin-1 receptors in rat cardiac tissue. (austin.org.au)
  • Endothelin-1, nitric oxide, and serotonin are related to blood pressure in adolescent males. (cusabio.com)
  • Objective -To compare the responses of equine digital arteries (EDAs) and equine digital veins (EDVs) to endothelin-1 (ET-1) and determine the role of the endothelium and type of receptors involved in the modulation and mediation of those responses, respectively. (avma.org)
  • Responses of EDAs and EDVs (with intact [+e] or denuded [-e] endothelium) to cumulative concentrations of ET-1 (10 -10 to 3 × 10 -7 M) were compared. (avma.org)
  • Endothelin (ET)-1 is a peptide produced mainly by the vascular endothelium. (arvojournals.org)
  • These agents competitively bind to endothelin-1 (ET-1) receptors ET A and ET B in endothelium and vascular smooth muscle, inhibiting vessel constriction and elevation of blood pressure. (medscape.com)
  • Conclusions and Implications These data support a novel role for ET-1 in the progression of sickle nephropathy, specifically via the ET A receptor, and suggest a potential role for ET A receptor antagonism in a treatment strategy. (elsevier.com)
  • Increased cardiac sympathetic drive and reduced vagal modulation following endothelin receptor antagonism in healthy conscious rats. (shengsci.com)
  • Endothelin secretion is regulated at the gene level. (degruyter.com)
  • Publications: endothelin-1 prolongs the pgf2 -induced reduction in progesterone secretion by corpora lutea on day 9 of the estrous cycle in gilts. (pharmapdf.com)
  • Key Results In response to PKC stimulation, reactive oxygen species production by isolated glomeruli from HbSS sickle mice was increased compared with that from HbSA controls, an effect that was prevented by 1 week in vivo treatment with the selective ET A antagonist, ABT-627. (elsevier.com)
  • Since the role of the Kv1.7 channel in PAH has not been previously studied, we investigated whether Kv1.7 channel expression changes in the lung tissue of a monocrotaline (MCT)-induced PAH rat model and whether this change is influenced by the endothelin (ET)-1 and reactive oxygen species (ROS) pathways. (ewha.ac.kr)
  • Both the precursor Big ET-1 and the shorter 21 aminoacid vasoactive form Endothelin-1 circulate in blood. (bmgrp.com)
  • Pulse pressure and urinary endothelin-1 (ET-1) and arginine vasopressin (AVP) vasoactive factors involved in the transitional circulation were measured before and after the NSAIDs treatment of 46 RDS premature infants receiving either ibuprofen (n = 22) or indomethacin (n = 24), with 28 responders and 18 nonresponders to the first NSAIDs course. (unipd.it)
  • Rings were subjected to exogenous contractile agonists (acetylcholine, histamine, endothelin-1, substance P, acetyl-substance P, and neurokinin A) or to electrical field stimulation (EFS) to differentiate cholinergic or nonadrenergic, noncholinergic nerve-mediated contraction with or without cumulatively increasing concentrations of propofol, thiopental, etomidate, or ketamine. (asahq.org)
  • Both PD98059 and U0126, inhibitors of the upstream activator of mitogen-activated protein kinase kinase, inhibited augmentation of endothelin-1 expression stimulated with leptin. (elsevier.com)
  • 2,3 VEGF signaling pathway inhibitors (VSPi) take advantage of tumor cells' dependence on blood supply by inhibiting VEGF signaling through various mechanisms of action: VEGF antibodies (e.g., bevacizumab), VEGFR antibodies (e.g., ramucirumab), and VEGFR TKIs (e.g., sorafenib, sunitinib) ( Table 1 ). (acc.org)
  • Open up in another window Physique 1 2D constructions from the kinase inhibitors profiled with this study.Each is kinase inhibitors which were approved for clinical make use of in Nov. 2013. (conferencedequebec.org)
  • Desk 1 Summary of promoted kinase inhibitors, their applications and biochemical features. (conferencedequebec.org)
  • On the other hand, most kinase inhibitors demonstrated a 100-fold difference, and dasatinib a good a lot more than 1000-fold difference Endothelin-2, human manufacture (Number 2D), demonstrating that kinase inhibitors certainly achieve a better selectivity window compared to traditional chemotherapeutic agencies. (conferencedequebec.org)
  • Inhibition of endothelin (ET) system in combination with established RAASis may represent such an approach. (nih.gov)
  • Furthermore, inhibition of the biological effects of Big ET by phosphoramidon is not via either direct or indirect antagonism of ET-1 thus supporting the idea that a unique, yet unidentified, metalloprotease is involved in producing the biological effects of Big ET, possibly by the specific conversion of Big ET to ET-1. (uab.edu)
  • However, the info show that is true because of Endothelin-2, human manufacture its inhibition of VEGFR2, a focus on of angiogenic medications, however, not for PDGFR, a focus Endothelin-2, human manufacture on in gastro-intestinal stromal tumours, a sign that regorafenib Rabbit Polyclonal to OR2B2 is accepted aswell (Desk 1). (conferencedequebec.org)
  • Big ET-1 is a 38 amino acid peptide and is the precursor of Endothelin-1 (ET-1). (bmgrp.com)
  • These results clearly indicate that the elimination of ET-1 from circulating blood and the ET-1-induced pressor response are not in parallel, and the relatively rapid disappearance of ET-1 from the bloodstream is mostly due to the removal of the peptide by the parenchymal tissues, in the anesthetized rat. (elsevier.com)
  • Conclusions and Clinical Relevance -Endothelin-1 induced digital vasoconstriction (marked constriction in veins). (avma.org)
  • The favorable effect of ghrelin on endothelin A-dependent vasoconstriction was likely related to the stimulation of NO production, because no change in the vascular effect of BQ-123 was observed after ghrelin (P=0.44) in 5 patients with metabolic syndrome during continuous infusion of the NO donor sodium nitroprusside (0.2 microg/min). (unicatt.it)
  • Acute aortic dissection is a rare but life-threatening condition with a lethality rate of 1 to 2% per hour after onset of symptoms in untreated patients. (smw.ch)
  • The incidence of acute aortic syndromes in the general population ranges from 4 to 6 cases per 100 000 person-years, but increases up to 30 or more in people older than 65 years [ 1 - 3 ]. (smw.ch)
  • With respect to the time from the onset of the symptoms, aortic dissections are divided into acute (presentation within 1 week), subacute (from 1 week to 1 month) and chronic (more than 1 month). (smw.ch)
  • Interven- infection with severe acute respiratory syndrome coro- tions for acute SCLS episodes are limited to support- navirus2.PersonswithknownorsuspectedSCLSmay ive measures, but monthly prophylaxis with high beatincreasedriskfordevelopingadiseaseflareinthe dose (1-2 g/kg patient weight) IV immunoglobulin settingofmild-to-moderateCOVID-19infection. (cdc.gov)
  • In this study, we evaluated the effects of amlodipine and/or a high cholesterol diet on the blood and aortic concentration of endothelin in rabbits. (ijp-online.com)
  • Amlodipine treatment reduced the levels of total cholesterol, LDL, and TG and, in a high lipid intake situation reduced endothelin levels in plasma and aortic tissue. (ijp-online.com)
  • In this study, we found that leptin induced extracellular signal-regulated kinase phosphorylation and endothelin-1 expression in rat aortic smooth muscle cells. (elsevier.com)
  • According to the more popular Stanford system, dissections involving the ascending aorta are classified as type A, whereas those involving only the descending aorta are classified as type B. The older DeBakey system differentiates between dissections evolving from the ascending aorta and affecting all aortic segments (type I), less extensive ones affecting only the ascending fragment (type II), and dissections affecting only descending aorta (type III) ( fig. 1 ). (smw.ch)
  • The results of this study indicated that ET-1 and VCAM-1 may be assessed together as markers of inflammation and the identification of patients at high risk for disease progression. (degruyter.com)
  • Serum levels of ICAM-1, VCAM-1 and ET-1 were assessed by enzyme immunoassay. (degruyter.com)
  • Determination of soluble adhesion molecules and ET-1 in serum SSc patients could be one of the laboratory markers for evaluating SSc activity and disease prognosis. (degruyter.com)
  • Big ET-1 can easily be measured using in serum and plasma with only 50µl sample volume. (bmgrp.com)
  • The release of cytokines/chemokines (interleukins-1α, 1-β (IL-1β), -6 (IL-6), -10 (IL-10), monocyte chemoattractant protein (MCP-1/CCL2), fractalkine and tissue inhibitor of metalloproteinases-1 (TIMP-1)) were simultaneously measured in brain and serum samples using the Agilent Technology cytokine microarray. (biomedcentral.com)
  • There was a trend for increased serum endothelin-1. (cdc.gov)
  • Als Voraussetzung einer Interaktion zwischen dem Transkriptionsfaktor Nkx2.5 und den alternativen Promotoren des ECE-1 wurde zunächst die Koexpression auf Protein- (Nkx2.5) und mRNA-Ebene (Nkx2.5, ECE-1-Isoformen) in einer Kardiomyoblastenzellinie, H9c2, nachgewiesen. (fu-berlin.de)
  • Die Wechselwirkung mit den alternativen ECE-1-Promotoren scheint dabei über unterschiedlich Mechanismen, teils direkt - für ECE-1b - und teils indirekt - für ECE-1a und -1c - vermittelt zu sein, was durch die Einführung von Mutationen in die Nkx2.5-Konsensussequenzen und durch Untersuchung der Protein-DNA-Interaktion mittels Bandshift-Analyse nachgewiesen werden konnte. (fu-berlin.de)
  • As a prerequisite for the interaction of the transcritpion factor Nkx2.5 and the alternative promotors of ECE-1 we gave evidence on protein (Nkx2.5) and on mRNA level (Nkx2.5, ECE-1 isoforms) for a coexpression in rat H9c2 cardiomyoblasts and on mRNA level in embryonic rat heart and heart tissue of patients with congenital heart disease. (fu-berlin.de)
  • In a previous study, we have shown that endothelin-1 (ET-1) activates phospholipase D independently from protein kinase C in osteoblast-like MC3T3- E1 cells. (fujita-hu.ac.jp)
  • The binding of IQ 1 to PR72/130 leads to decreased phosphorylation of the coactivator protein p300 at Ser-89. (xcessbio.com)
  • No associations between ET-1 and ICAM-1 concentrations were detected. (degruyter.com)
  • Depending on the duration of the disease no significant differences in the concentrations of ET-1, ICAM-1 and VCAM-1 were detected. (degruyter.com)
  • ET-1 and big ET-1 are found in equimolar concentrations in the plasma. (bmgrp.com)
  • Exploratory models were additionally adjusted for hemoglobin and endothelin-1 concentrations. (asn-online.org)
  • This occurs through stimulation of six steps in thyroid hormone synthesis: (1) Up-regulating the activity of the sodium-iodide symporter (NIS) on the basolateral membrane of follicular cells , thereby increasing intracellular concentrations of iodine (iodine trapping). (wikidoc.org)
  • Endothelin family has three endothelin isoforms, ET-1, ET-2 and ET-3. (degruyter.com)
  • Using luciferase reporter gene assays, site-directed mutagenesis and gel shift assays we showed that Nkx2.5 differentially regulates the alternative promotors of ECE-1 isoforms. (fu-berlin.de)
  • 4. COVID-19 infection confirmed by laboratory tests (polymerase chain reaction testing, enzyme-linked immunosorbent assay (positive result at least 1 time) with a CT degree more that 25% of lung lession. (who.int)
  • Predictive Value of Plasma Big Endothelin-1 in Adverse Events of Patients With Coronary Artery Restenosis and Diabetes Mellitus: Beyond Traditional and Angiographic Risk Factors. (bmgrp.com)
  • A 38 amino acid form of endothelin-1 that results from alternative processing of proendothelin-1. (bvsalud.org)
  • Endothelins are a family of 21-amino acid oligopeptides, called endothelin-1 (ET-1), endothelin-2 (ET-2), and endothelin 3 (ET-3). (istun.edu.tr)
  • Mouse knock-out models have established a fundamental role for the transcription factor Nkx2.5 and for the metalloprotease, endothelin- converting-enzyme-1 (ECE-1), in heart development. (fu-berlin.de)
  • Simultaneous intravenous infusion of phosphoramidon (0.25 mg · kg-1 · min-1), an inhibitor of metalloprotease activity including neutral endopeptidase EC (NEP), completely prevented these effects of Big ET. (uab.edu)
  • Similarly, the response to Big ET was unaffected by infusion of enalaprilat (0.1 mg · kg-1 · min-1), an inhibitor of the angiotensin-converting enzyme, which is also a metalloprotease. (uab.edu)
  • The analysis of the chemical form of labeled peptides from the plasma by reverse-phase high-performance liquid chromatography (HPLC) demonstrated no appreciable amount of degraded forms of [ 125 I]-ET-1 in the blood for up to 60 min. (elsevier.com)
  • Endothelin-1 regulates cardiac sympathetic innervation in the rodent heart by controlling nerve growth factor expression. (nii.ac.jp)
  • These results indicate that the hemodynamic effects of Big ET and ET-1 display different potencies in terms of the renal vs. systemic circulation. (uab.edu)
  • These results strongly suggest that phosphatidylcholine hydrolysis by phospholipase D is involved in the arachidonic acid release induced by ET-1 in osteoblast-like cells. (fujita-hu.ac.jp)
  • Our results suggest that ET-1 plays a role in IH-induced impairments in glucose homeostasis. (figshare.com)
  • 1 Because PH is uncommon and there is limited awareness, most patients receive the diagnosis late in the disease course, which results in delayed initiation of effective therapies, greater patient suffering and potentially worse long-term clinical outcomes, including survival. (cmaj.ca)
  • In 2012 proteins kinases had been the solitary most successful focus on class predicated on the amount of authorized new medicines from the U.S. Meals and Medication Administration (FDA) which trend continuing in 2013 [1]. (conferencedequebec.org)
  • a IL-1 gene manifestation was considerably less pronounced in PKRA7-treated mice (ideals by Mann-Whitney check Discussion In today's study, we exhibited that PKR1 proteins was indicated in infiltrating neutrophils, while PKR2 proteins was within macrophage-like mononuclear cells in the synovial membrane of CIA mice. (exposed-skin-care.net)
  • A clinical study in 8550 patients investigated the association between the cardio-vascular marker big endothelin-1 (big ET-1) and long-term all-cause death in patients with coronary artery disease (CAD) and impaired glucose metabolism. (bmgrp.com)
  • Patients were categorized into both glucose status (diabetes mellitus, pre-diabetes mellitus, normalglycemia) and big ET-1 level groups. (bmgrp.com)
  • The data indicate that baseline big ET-1 levels were independently associated with the long-term mortality in diabetes patients with CAD. (bmgrp.com)
  • The present study aimed to examine the association between big endothelin-1 (big ET-1) and long-term all-cause death in patients with coronary artery disease (CAD) and different glucose metabolism status. (bmgrp.com)
  • Patients were categorized according to both status of glucose metabolism status [Diabetes Mellitus (DM), Pre-Diabetes (Pre-DM), Normoglycemia (NG)] and big ET-1 levels. (bmgrp.com)
  • The present data indicate that baseline big ET-1 levels were independently associated with the long-term all-cause death in DM and Pre-DM patients with CAD undergoing PCI, suggesting that big ET-1 may be a valuable marker in patients with impaired glucose metabolism. (bmgrp.com)
  • Baseline plasma ET-1 levels were similar between patients with glaucoma and control subjects (mean ± SD: 2.81 ± 1.29 and 2.56 ± 1.36 pg/mL, respectively, P = 0.465). (arvojournals.org)
  • Patients with glaucoma, however, had a significant increase in plasma ET-1 after cooling (mean ± SD increase of 34% ± 52%, P = 0.001), not observed in control subjects (mean ± SD increase of 7% ± 43%, P = 0.750). (arvojournals.org)
  • Patients with glaucoma have an abnormal increase in plasma ET-1 after the body cools. (arvojournals.org)
  • It is possible that at least in some patients, increased levels of ET-1 in response to vasospastic stimuli may be involved in the pathogenesis of glaucomatous damage. (arvojournals.org)
  • 1 5 6 7 8 A recent study has also identified migraine as an important risk factor associated with progression of the disease in patients with untreated normal-tension glaucoma. (arvojournals.org)
  • [ 34 , 35 ] In a controlled study of 70 patients treated with these agents, approximately 50% maintained actual long-term New York Heart Association (NYHA) functional class improvement at 1 year, without the need for another treatment. (medscape.com)
  • [ 38 ] Another trial, in which a cohort of 162 patients was studied after 1 year of receiving epoprostenol therapy, confirmed that patients' clinical function improved significantly, even though improvements in hemodynamic measures were modest. (medscape.com)
  • Therefore, we tested whether exogenous ghrelin may have benefits to improve the balance between endothelin 1 and NO in patients with obesity-related metabolic syndrome. (unicatt.it)
  • It is estimated that the number of glaucoma patients will increase in the future ( 1 , 2 ). (frontiersin.org)
  • Background and Purpose Endothelin-1 (ET-1) is increased in patients with sickle cell disease and may contribute to the development of sickle cell nephropathy. (elsevier.com)
  • Elevated endothelin-1 (ET-1) levels have been observed in OSA patients and in mice exposed to intermittent hypoxia (IH). (figshare.com)
  • Background: Diabetes mellitus type 1 leads to various complications which make diabetic patients anxious. (endocrine-abstracts.org)
  • In this study, anxieties of 11 diabetic patients who could take their blood sugar under control were investigated and solutions were suggested and done.Patients and methods: Eleven patients with diabetes mellitus type 1 listed their anxieties and ranked them in matris. (endocrine-abstracts.org)
  • Epithelial-derived endothelin-1 and fibroblast growth factor were also augmented in smad2-expressing mice. (ox.ac.uk)
  • Open in a separate window Number 1 Fibroblast growth element 10 (FGF10) enhances engine and sensory practical recovery after peripheral nerve injury (PNI). (bios-mep.info)
  • In addition to modulating vascular tone and extracellular matrix turnover, ET-1 up-regulates cell surface adhesion molecules-intercellular adhesion molecule-1 (ICAM-1) and vascular cell adhesion molecule-1 (VCAM-1).The aim of the study was to evaluate the diagnostic value of the detection of ET-1, VCAM-1 and ICAM-1 in the diagnosis of systemic sclerosis. (degruyter.com)
  • Pretreatment of cells with AG1478 significantly reduced the degree of phosphorylation of extracellular signal-regulated kinase and endothelin-1 expression. (elsevier.com)
  • Observation of the [Ca(2+)](in) elevation in ND7/104 and HEK 2931 cells in the absence of extracellular calcium suggests that ET-1 elicits a release of calcium from intracellular stores, and pretreatment of the cells with pertussis toxin or a selective inhibitor of phospholipase C (PLC) point to a mechanism involving G alpha q/11 coupling. (archives-ouvertes.fr)
  • [6] ET-1 may contribute to the progression of several cardiovascular disorders such as congestive heart failure, hypertension, and ischemic heart disease. (ijp-online.com)
  • Endobloc 10 mg Tablet is an antihypertensive medication explicitly utilized in the treatment of pneumonic blood vessel hypertension (PAH) (WHO class 1), a condition portrayed by hypertension in the vessels conveying blood from the heart to the lungs. (cheapmedicinepills.com)
  • A series of clinical scenarios centered on 1 or the 3 etiologic groups (IPAH, CTD-associated PAH, and portopulmonary hypertension) were presented to the panelists for the development of the consensus. (pulmonologyadvisor.com)
  • Endothelin 1 mRNA levels in the lungs of PHB were significantly higher than the corresponding level in NPHB (P (eurekamag.com)
  • In contrast, the opposite was true for ET-1 type A receptor mRNA levels (P (eurekamag.com)
  • Experimental Approach Adult, humanized HbSS (homozygous for sickle Hb) mice had increased ET-1 mRNA expression in both the cortex and the glomeruli compared with mice heterozygous for sickle and Hb A (HbAS controls). (elsevier.com)
  • Furthermore, reduction of ET(B) mRNA levels by siRNA does not abrogate calcium mobilization by ET-1 in HEK 293T cells, corroborating the lack of an ET(B) receptor role in this response. (archives-ouvertes.fr)
  • However, in HEK 293 cells with low endogenous ET(A) mRNA levels, ET-1 does not induce a transient increase in [Ca(2+)](in). (archives-ouvertes.fr)
  • The subtractive mRNA hybridization followed by RT-PCR and immunoblotting revealed that down-regulation of Nedd4L significantly decreased the expression of collagenases matrix metalloproteinase (MMP)-1 and -13 in gallbladder cancer cells. (cancer-ecosystem.com)
  • Figure 1: Therapeutic principles of myocardial ischaemia. (nature.com)
  • Endothelin-1 (ET-1) has been implicated in the pathogenesis of inflammatory and fibrotic diseases, including systemic sclerosis. (degruyter.com)
  • This condition is believed to be brought about by expanded degrees of a specific characteristic substance (endothelin-1). (cheapmedicinepills.com)
  • It obstructs the activity of endothelin (a characteristic substance) that causes veins to limit (contract). (cheapmedicinepills.com)
  • 1 2 Indirect evidence has supported an association between vasospasm and glaucoma, including a high prevalence of vasospastic diseases, such as migraine, 3 4 and an abnormal peripheral reactivity to cold in glaucomatous eyes. (arvojournals.org)
  • Endothelin-1 directs airway remodeling and hyper-reactivity in a murine asthma model. (ox.ac.uk)
  • 1 The presumed mechanism of airway protection by propofol involves the attenuation of parasympathetic nerve acetylcholine release: the assumed mechanism of irritant-induced bronchoconstriction. (asahq.org)
  • [1] It is a glycoprotein hormone produced by thyrotrope cells in the anterior pituitary gland , which regulates the endocrine function of the thyroid . (wikidoc.org)
  • Blood samples from umbilical artery and maternal venous blood were collected at the time of delivery for analysis of ET-1 and leptin levels. (who.int)
  • Maternal plasma leptin and ET-1 levels may reflect deterioration in fetal growth. (who.int)
  • Preeclamptic plasma stimulates the expression of miRNAs in HUVECs, leading to a decrease in endothelin-1 levels. (cusabio.com)
  • However, uric acid and interleukin-1β levels in the lung were increased. (ox.ac.uk)
  • ET-1 levels remain elevated when NSAIDs fail to interrupt left-to-right PDA shunting that complicates recovery from RDS. (unipd.it)
  • Increased plasma levels of endothelin-like immunoreactivity during endotoxin administration within the pig. (edu.hk)
  • Thiorphan (0.1 mg · kg-1 · min-1), also an inhibitor of NEP, had absolutely no effect on either the renal or cardiovascular response to Big ET. (uab.edu)
  • The current study was designed to determine whether ET-1 acting via the ET A receptor contributes to renal injury in a mouse model of sickle cell disease. (elsevier.com)
  • MicroRNAs as markers to monitor endothelin-1 signalling and potential treatment in renal disease: Carcinoma - proteinuric damage - toxicity. (bvsalud.org)
  • 1. This study was designed to test the haemodynamic and renal effects in sheep of dihydrocyclosporin D (dCyD), an immunosuppressant agent derived from the fungus Tolypocladium inflatum Gams. (shengsci.com)
  • Blood was collected before and after cooling, and plasma ET-1 was determined by immunoassay. (arvojournals.org)
  • Maternal plasma ET-1 and leptin correlate with the degree of fetal growth restriction originating from deterioration of placental function. (who.int)
  • We show here that plasma immunoreactive en. (nsw.gov.au)
  • The plasma level of endothelin-1 in the atherosclerotic model group was significantly increased as compared to the control group ( P (ijp-online.com)
  • High cholesterol causes increase in plasma and tissue endothelin. (ijp-online.com)
  • After IH or IA exposure, insulin (0.5 IU/kg) or glucose (1 mg/kg) was injected intraperitoneally and plasma glucose determined after injection and area under glucose curve (AUC) was calculated. (figshare.com)
  • In ZDF rats, a single oral dose of CHIR 99021 (16 mg/kg or 48 mg/kg) rapidly lowers plasma glucose, with a maximal reduction of nearly 150 mg/dl 3-4 h after administration[1]. (dcchemicals.com)
  • 2018 May 1;98(5):287-289. (cdc.gov)
  • We examined whether pharmacological blockade of type A and type B ET-1 receptors (ET A and ET B ) would ameliorate glucose intolerance and IR in mice exposed to IH. (figshare.com)
  • IMSEAR at SEARO: Endothelin-1 and leptin as markers of intrauterine growth restriction. (who.int)
  • To determine whether the effect of phosphoramidon was due to antagonism of ET-1, an identical series of experiments was performed using ET-1 infusion (0.02 nmol · kg-1 · min-1). (uab.edu)
  • Regorafenib is certainly a structural analog Endothelin-2, human manufacture of sorafenib and displays an identical biochemical profile (Body 3A). (conferencedequebec.org)
  • In the present study, we investigated the role of phospholipase D activation in ET-1-induced arachidonic acid release and prostaglandin E 2 (PGE 2 ) synthesis in osteoblast-like MC3T3-E1 cells. (fujita-hu.ac.jp)
  • Vor dem Hintergrund der in der Literatur veröffentlichten Daten über die Expression von Nkx2.5 und ECE-1 im gesunden und insuffizienten Herzen unterstützen die Ergebnisse dieser Arbeit die Hypothese, daß Nkx2.5 auch in vivo ein entwicklungsbiologisch relevanter transkriptioneller Regulator der myokardialen ECE-1-Expression sein könnte. (fu-berlin.de)
  • Moreover, juvenile and adult brain showed differences in their expression profiles of cytokines and chemokines mediated by ET-1. (biomedcentral.com)
  • Examination of the expression of ET(A) and ET(B) receptors by RT-PCR and [(125)I]-ET-1 binding experiments confirms the slight predominance of ET(A) receptor binding sites and messenger RNA in both ND7/104 and HEK 293T cells. (archives-ouvertes.fr)
  • Conclusion: Decreased Kv1.7 channel expression might be caused by the ET-1 and ROS pathways and contributes to MCT-induced PAH. (ewha.ac.kr)
  • 1. It is well documented that cisplatin (CDDP) treatment increases the expression of adenosine A(1) receptors in both kidney and testes. (shengsci.com)