Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Cell surface proteins that bind ANGIOTENSINS and trigger intracellular changes influencing the behavior of cells.
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.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Agents that antagonize ANGIOTENSIN II TYPE 1 RECEPTOR. Included are ANGIOTENSIN II analogs such as SARALASIN and biphenylimidazoles such as LOSARTAN. Some are used as ANTIHYPERTENSIVE AGENTS.
An angiotensin receptor subtype that is expressed at high levels in a variety of adult tissues including the CARDIOVASCULAR SYSTEM, the KIDNEY, the ENDOCRINE SYSTEM and the NERVOUS SYSTEM. Activation of the type 1 angiotensin receptor causes VASOCONSTRICTION and sodium retention.
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.
Drugs used in the treatment of acute or chronic vascular HYPERTENSION regardless of pharmacological mechanism. Among the antihypertensive agents are DIURETICS; (especially DIURETICS, THIAZIDE); ADRENERGIC BETA-ANTAGONISTS; ADRENERGIC ALPHA-ANTAGONISTS; ANGIOTENSIN-CONVERTING ENZYME INHIBITORS; CALCIUM CHANNEL BLOCKERS; GANGLIONIC BLOCKERS; and VASODILATOR AGENTS.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
A BLOOD PRESSURE regulating system of interacting components that include RENIN; ANGIOTENSINOGEN; ANGIOTENSIN CONVERTING ENZYME; ANGIOTENSIN I; ANGIOTENSIN II; and angiotensinase. Renin, an enzyme produced in the kidney, acts on angiotensinogen, an alpha-2 globulin produced by the liver, forming ANGIOTENSIN I. Angiotensin-converting enzyme, contained in the lung, acts on angiotensin I in the plasma converting it to ANGIOTENSIN II, an extremely powerful vasoconstrictor. Angiotensin II causes contraction of the arteriolar and renal VASCULAR SMOOTH MUSCLE, leading to retention of salt and water in the KIDNEY and increased arterial blood pressure. In addition, angiotensin II stimulates the release of ALDOSTERONE from the ADRENAL CORTEX, which in turn also increases salt and water retention in the kidney. Angiotensin-converting enzyme also breaks down BRADYKININ, a powerful vasodilator and component of the KALLIKREIN-KININ SYSTEM.
An angiotensin receptor subtype that is expressed at high levels in fetal tissues. Many effects of the angiotensin type 2 receptor such as VASODILATION and sodium loss are the opposite of that of the ANGIOTENSIN TYPE 1 RECEPTOR.
A decapeptide that is cleaved from precursor angiotensinogen by RENIN. Angiotensin I has limited biological activity. It is converted to angiotensin II, a potent vasoconstrictor, after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME.
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.
PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS.
A heptapeptide formed from ANGIOTENSIN II after the removal of an amino acid at the N-terminal by AMINOPEPTIDASE A. Angiotensin III has the same efficacy as ANGIOTENSIN II in promoting ALDOSTERONE secretion and modifying renal blood flow, but less vasopressor activity (about 40%).
Compounds with a BENZENE fused to IMIDAZOLES.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
Agents that antagonize the ANGIOTENSIN II TYPE 2 RECEPTOR.
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.
Oligopeptides which are important in the regulation of blood pressure (VASOCONSTRICTION) and fluid homeostasis via the RENIN-ANGIOTENSIN SYSTEM. These include angiotensins derived naturally from precursor ANGIOTENSINOGEN, and those synthesized.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
The relationship between the dose of an administered drug and the response of the organism to the drug.
An ANGIOTENSIN II analog which acts as a highly specific inhibitor of ANGIOTENSIN TYPE 1 RECEPTOR.
A branched-chain essential amino acid that has stimulant activity. It promotes muscle growth and tissue repair. It is a precursor in the penicillin biosynthetic pathway.
An octapeptide analog of angiotensin II (bovine) with amino acids 1 and 8 replaced with sarcosine and alanine, respectively. It is a highly specific competitive inhibitor of angiotensin II that is used in the diagnosis of HYPERTENSION.
Derivatives of BENZOIC ACID. Included under this heading are a broad variety of acid forms, salts, esters, and amides that contain the carboxybenzene structure.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
A peptidyl-dipeptidase that catalyzes the release of a C-terminal dipeptide, -Xaa-*-Xbb-Xcc, when neither Xaa nor Xbb is Pro. It is a Cl(-)-dependent, zinc glycoprotein that is generally membrane-bound and active at neutral pH. It may also have endopeptidase activity on some substrates. (From Enzyme Nomenclature, 1992) EC 3.4.15.1.
A highly specific (Leu-Leu) endopeptidase that generates ANGIOTENSIN I from its precursor ANGIOTENSINOGEN, leading to a cascade of reactions which elevate BLOOD PRESSURE and increase sodium retention by the kidney in the RENIN-ANGIOTENSIN SYSTEM. The enzyme was formerly listed as EC 3.4.99.19.
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.
Drugs used to cause constriction of the blood vessels.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
A family of hexahydropyridines.
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Therapy with two or more separate preparations given for a combined effect.
Compounds based on fumaric acid.
A hormone secreted by the ADRENAL CORTEX that regulates electrolyte and water balance by increasing the renal retention of sodium and the excretion of potassium.
One of the ANGIOTENSIN-CONVERTING ENZYME INHIBITORS (ACE inhibitors), orally active, that has been used in the treatment of hypertension and congestive heart failure.
Cell surface proteins that bind ENDOTHELINS with high affinity and trigger intracellular changes which influence the behavior of cells.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
An angiotensin-converting enzyme inhibitor that is used to treat HYPERTENSION and HEART FAILURE.
Agents that promote the excretion of urine through their effects on kidney function.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
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 that bind to but do not activate beta-adrenergic receptors thereby blocking the actions of beta-adrenergic agonists. Adrenergic beta-antagonists are used for treatment of hypertension, cardiac arrhythmias, angina pectoris, glaucoma, migraine headaches, and anxiety.
Compounds with BENZENE fused to AZEPINES.
The presence of proteins in the urine, an indicator of KIDNEY DISEASES.
Agents inhibiting the effect of narcotics on the central nervous system.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
A long-acting dihydropyridine calcium channel blocker. It is effective in the treatment of ANGINA PECTORIS and HYPERTENSION.
A potassium sparing diuretic that acts by antagonism of aldosterone in the distal renal tubules. It is used mainly in the treatment of refractory edema in patients with congestive heart failure, nephrotic syndrome, or hepatic cirrhosis. Its effects on the endocrine system are utilized in the treatments of hirsutism and acne but they can lead to adverse effects. (From Martindale, The Extra Pharmacopoeia, 30th ed, p827)
An alpha-globulin of about 453 amino acids, depending on the species. It is produced by the liver and secreted into blood circulation. Angiotensinogen is the inactive precursor of natural angiotensins. Upon successive enzyme cleavages, angiotensinogen yields angiotensin I, II, and III with amino acids numbered at 10, 8, and 7, respectively.
A strain of Rattus norvegicus with elevated blood pressure used as a model for studying hypertension and stroke.
The physiological narrowing of BLOOD VESSELS by contraction of the VASCULAR SMOOTH MUSCLE.
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.
Elements of limited time intervals, contributing to particular results or situations.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
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.
A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
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.
A subtype of endothelin receptor found predominantly in the VASCULAR SMOOTH MUSCLE. It has a high affinity for ENDOTHELIN-1 and ENDOTHELIN-2.
A long-acting angiotensin-converting enzyme inhibitor. It is a prodrug that is transformed in the liver to its active metabolite ramiprilat.
A thiazide diuretic often considered the prototypical member of this class. It reduces the reabsorption of electrolytes from the renal tubules. This results in increased excretion of water and electrolytes, including sodium, potassium, chloride, and magnesium. It is used in the treatment of several disorders including edema, hypertension, diabetes insipidus, and hypoparathyroidism.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
The nonstriated involuntary muscle tissue of blood vessels.
A strain of Rattus norvegicus used as a normotensive control for the spontaneous hypertensive rats (SHR).
Peptides composed of between two and twelve amino acids.
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 class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
An inhibitor of glutamate decarboxylase. It decreases the GAMMA-AMINOBUTYRIC ACID concentration in the brain, thereby causing convulsions.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
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.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.
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)
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.
Evaluation undertaken to assess the results or consequences of management and procedures used in combating disease in order to determine the efficacy, effectiveness, safety, and practicability of these interventions in individual cases or series.
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.
A diet which contains very little sodium chloride. It is prescribed by some for hypertension and for edematous states. (Dorland, 27th ed)
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
Organic compounds containing the -CO-NH2 radical. Amides are derived from acids by replacement of -OH by -NH2 or from ammonia by the replacement of H by an acyl group. (From Grant & Hackh's Chemical Dictionary, 5th ed)
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Pathological processes of the KIDNEY or its component tissues.
KIDNEY injuries associated with diabetes mellitus and affecting KIDNEY GLOMERULUS; ARTERIOLES; KIDNEY TUBULES; and the interstitium. Clinical signs include persistent PROTEINURIA, from microalbuminuria progressing to ALBUMINURIA of greater than 300 mg/24 h, leading to reduced GLOMERULAR FILTRATION RATE and END-STAGE RENAL DISEASE.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
A method of studying a drug or procedure in which both the subjects and investigators are kept unaware of who is actually getting which specific treatment.
The circulation of the BLOOD through the vessels of the KIDNEY.
Abnormally high potassium concentration in the blood, most often due to defective renal excretion. It is characterized clinically by electrocardiographic abnormalities (elevated T waves and depressed P waves, and eventually by atrial asystole). In severe cases, weakness and flaccid paralysis may occur. (Dorland, 27th ed)
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 statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
The active metabolite of ENALAPRIL and a potent intravenously administered angiotensin-converting enzyme inhibitor. It is an effective agent for the treatment of essential hypertension and has beneficial hemodynamic effects in heart failure. The drug produces renal vasodilation with an increase in sodium excretion.
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.
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 group of compounds that contain the structure SO2NH2.
The number of times the HEART VENTRICLES contract per unit of time, usually per minute.
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.
The movement and the forces involved in the movement of the blood through the CARDIOVASCULAR SYSTEM.
Purine bases found in body tissues and fluids and in some plants.
A direct-acting vasodilator that is used as an antihypertensive agent.
Agents that affect the rate or intensity of cardiac contraction, blood vessel diameter, or blood volume.
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).
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
Injections into the cerebral ventricles.
Persistent high BLOOD PRESSURE due to KIDNEY DISEASES, such as those involving the renal parenchyma, the renal vasculature, or tumors that secrete RENIN.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
The main trunk of the systemic arteries.
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)
A constitutively expressed subtype of bradykinin receptor that may play a role in the acute phase of the inflammatory and pain response. It has high specificity for intact forms of BRADYKININ and KALLIDIN. The receptor is coupled to G-PROTEIN, GQ-G11 ALPHA FAMILY and G-PROTEIN, GI-GO ALPHA FAMILY signaling proteins.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
A subtype of endothelin receptor found predominantly in the KIDNEY. It may play a role in reducing systemic ENDOTHELIN levels.
The thoracolumbar division of the autonomic nervous system. Sympathetic preganglionic fibers originate in neurons of the intermediolateral column of the spinal cord and project to the paravertebral and prevertebral ganglia, which in turn project to target organs. The sympathetic nervous system mediates the body's response to stressful situations, i.e., the fight or flight reactions. It often acts reciprocally to the parasympathetic system.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
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 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 biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
Seven membered heterocyclic rings containing a NITROGEN atom.
Works about clinical trials that involve at least one test treatment and one control treatment, concurrent enrollment and follow-up of the test- and control-treated groups, and in which the treatments to be administered are selected by a random process, such as the use of a random-numbers table.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
The physiological widening of BLOOD VESSELS by relaxing the underlying VASCULAR SMOOTH MUSCLE.
Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
Single pavement layer of cells which line the luminal surface of the entire vascular system and regulate the transport of macromolecules and blood components.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
Use of electric potential or currents to elicit biological responses.
A potent and specific inhibitor of PEPTIDYL-DIPEPTIDASE A. It blocks the conversion of ANGIOTENSIN I to ANGIOTENSIN II, a vasoconstrictor and important regulator of arterial blood pressure. Captopril acts to suppress the RENIN-ANGIOTENSIN SYSTEM and inhibits pressure responses to exogenous angiotensin.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
The volume of water filtered out of plasma through glomerular capillary walls into Bowman's capsules per unit of time. It is considered to be equivalent to INULIN clearance.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
A non-selective inhibitor of nitric oxide synthase. It has been used experimentally to induce hypertension.
Enlargement of the HEART, usually indicated by a cardiothoracic ratio above 0.50. Heart enlargement may involve the right, the left, or both HEART VENTRICLES or HEART ATRIA. Cardiomegaly is a nonspecific symptom seen in patients with chronic systolic heart failure (HEART FAILURE) or several forms of CARDIOMYOPATHIES.
A selective serotonin receptor antagonist with weak adrenergic receptor blocking properties. The drug is effective in lowering blood pressure in essential hypertension. It also inhibits platelet aggregation. It is well tolerated and is particularly effective in older patients.
The observable response an animal makes to any situation.
A nucleoside that is composed of ADENINE and D-RIBOSE. Adenosine or adenosine derivatives play many important biological roles in addition to being components of DNA and RNA. Adenosine itself is a neurotransmitter.
The hollow, muscular organ that maintains the circulation of the blood.
The presence of albumin in the urine, an indicator of KIDNEY DISEASES.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
Any pathological condition where fibrous connective tissue invades any organ, usually as a consequence of inflammation or other injury.
Drugs that bind to but do not activate ADRENERGIC RECEPTORS. Adrenergic antagonists block the actions of the endogenous adrenergic transmitters EPINEPHRINE and NOREPINEPHRINE.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
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).
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.
An amine derived by enzymatic decarboxylation of HISTIDINE. It is a powerful stimulant of gastric secretion, a constrictor of bronchial smooth muscle, a vasodilator, and also a centrally acting neurotransmitter.
A member of the alkali group of metals. It has the atomic symbol Na, atomic number 11, and atomic weight 23.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
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.
A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.
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.
Sodium chloride used in foods.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
The vessels carrying blood away from the heart.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
The rate dynamics in chemical or physical systems.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
The octapeptide amide of bovine angiotensin II used to increase blood pressure by vasoconstriction.
The largest family of cell surface receptors involved in SIGNAL TRANSDUCTION. They share a common structure and signal through HETEROTRIMERIC G-PROTEINS.
An isoquinoline alkaloid obtained from Dicentra cucullaria and other plants. It is a competitive antagonist for GABA-A receptors.
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.
Sodium or sodium compounds used in foods or as a food. The most frequently used compounds are sodium chloride or sodium glutamate.
The lower portion of the BRAIN STEM. It is inferior to the PONS and anterior to the CEREBELLUM. Medulla oblongata serves as a relay station between the brain and the spinal cord, and contains centers for regulating respiratory, vasomotor, cardiac, and reflex activities.
CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.
Single preparations containing two or more active agents, for the purpose of their concurrent administration as a fixed dose mixture.

Irbesartan reduces QT dispersion in hypertensive individuals. (1/1416)

Angiotensin type 1 receptor antagonists have direct effects on the autonomic nervous system and myocardium. Because of this, we hypothesized that irbesartan would reduce QT dispersion to a greater degree than amlodipine, a highly selective vasodilator. To test this, we gathered electrocardiographic (ECG) data from a multinational, multicenter, randomized, double-blind parallel group study that compared the antihypertensive efficacy of irbesartan and amlodipine in elderly subjects with mild to moderate hypertension. Subjects were treated for 6 months with either drug. Hydrochlorothiazide and atenolol were added after 12 weeks if blood pressure (BP) remained uncontrolled. ECGs were obtained before randomization and at 6 months. A total of 188 subjects (118 with baseline ECGs) were randomized. We analyzed 104 subjects who had complete ECGs at baseline and after 6 months of treatment. Baseline characteristics between treatments were similar, apart from a slight imbalance in diastolic BP (irbesartan [n=53] versus amlodipine [n=51], 99.2 [SD 3. 6] versus 100.8 [3.8] mm Hg; P=0.03). There were no significant differences in BP normalization (diastolic BP <90 mm Hg) between treatments at 6 months (irbesartan versus amlodipine, 80% versus 88%; P=0.378). We found a significant reduction in QT indexes in the irbesartan group (QTc dispersion mean, -11.4 [34.5] milliseconds, P=0.02; QTc max, -12.8 [35.5] milliseconds, P=0.01), and QTc dispersion did not correlate with the change in BP. The reduction in QT indexes with amlodipine (QTc dispersion, -9.7 [35.4] milliseconds, P=0.06; QTc max, -8.6 [33.2] milliseconds, P=0.07) did not quite reach statistical significance, but there was a correlation between the change in QT indexes and changes in systolic BP. In conclusion, irbesartan improved QT dispersion, and this effect may be important in preventing sudden cardiac death in at-risk hypertensive subjects.  (+info)

Angiotensin receptor subtype 1 mediates angiotensin II enhancement of isoproterenol-induced cyclic AMP production in preglomerular microvascular smooth muscle cells. (2/1416)

In a previous study, we found that angiotensin (Ang) II enhances beta-adrenoceptor-induced cAMP production in cultured preglomerular microvascular smooth muscle cells (PMVSMCs) obtained from spontaneously hypertensive rats. The purpose of the present investigation was to identify the Ang receptor subtypes that mediate this effect. In our first study, we compared the ability of Ang II, Ang III, Ang (3-8), and Ang (1-7) to increase cAMP production in isoproterenol (1 microM)-treated PMVSMCs. Each peptide was tested at 0.1, 1, 10, 100, and 1000 nM. Both Ang II and Ang III increased intracellular (EC50s, 1 and 11 nM, respectively) and extracellular (EC50s, 2 and 14 nM, respectively) cAMP levels in a concentration-dependent fashion. In contrast, Ang (3-8) and Ang (1-7) did not enhance either intracellular or extracellular cAMP levels at any concentration tested. In our second study, we examined the ability of L 158809 [a selective Ang receptor subtype 1 (AT1) receptor antagonist] to inhibit Ang II (100 nM) and Ang III (100 nM) enhancement of isoproterenol (1 microM)-induced cAMP production in PMVSMCs. L 158809 (10 nM) abolished or nearly abolished (p <.001) Ang II and Ang III enhancement of isoproterenol-induced intracellular and extracellular cAMP levels. In contrast, PD 123319 (300 nM; a selective AT2 receptor antagonist) did not significantly alter Ang II enhancement of isoproterenol-induced intracellular or extracellular cAMP levels. We conclude that AT1 receptors, but not AT2, Ang (3-8), nor Ang (1-7) receptors mediate Ang II and Ang III enhancement of beta-adrenoceptor-induced cAMP production in cultured PMVSMCs.  (+info)

Blocking angiotensin II ameliorates proteinuria and glomerular lesions in progressive mesangioproliferative glomerulonephritis. (3/1416)

BACKGROUND: The renin-angiotensin system is thought to be involved in the progression of glomerulonephritis (GN) into end-stage renal failure (ESRF) because of the observed renoprotective effects of angiotensin-converting enzyme inhibitors (ACEIs). However, ACEIs have pharmacological effects other than ACE inhibition that may help lower blood pressure and preserve glomerular structure. We previously reported a new animal model of progressive glomerulosclerosis induced by a single intravenous injection of an anti-Thy-1 monoclonal antibody, MoAb 1-22-3, in uninephrectomized rats. Using this new model of progressive GN, we examined the hypothesis that ACEIs prevent the progression to ESRF by modulating the effects of angiotensin II (Ang II) on the production of transforming growth factor-beta (TGF-beta) and extracellular matrix components. METHODS: We studied the effect of an ACEI (cilazapril) and an Ang II type 1 receptor antagonist (candesartan) on the clinical features and morphological lesions in the rat model previously reported. After 10 weeks of treatment with equihypotensive doses of cilazapril, cilazapril plus Hoe 140 (a bradykinin receptor B2 antagonist), candesartan, and hydralazine, we examined systolic blood pressure, urinary protein excretion, creatinine clearance, the glomerulosclerosis index, and the tubulointerstitial lesion index. We performed a semiquantitative evaluation of glomerular immunostaining for TGF-beta and collagen types I and III by immunofluorescence study and of these cortical mRNA levels by Northern blot analysis. RESULTS: Untreated rats developed massive proteinuria, renal dysfunction, and severe glomerular and tubulointerstitial injury, whereas uninephrectomized control rats did not. There was a significant increase in the levels of glomerular protein and cortical mRNA for TGF-beta and collagen types I and III in untreated rats. Cilazapril and candesartan prevented massive proteinuria, increased creatinine clearance, and ameliorated glomerular and tubulointerstitial injury. These drugs also reduced levels of glomerular protein and cortical mRNA for TGF-beta and collagen types I and III. Hoe 140 failed to blunt the renoprotective effect of cilazapril. Hydralazine did not exhibit a renoprotective effect. CONCLUSION: These results indicate that ACEIs prevent the progression to ESRF by modulating the effects of Ang II via Ang II type 1 receptor on the production of TGF-beta and collagen types I and III, as well as on intrarenal hemodynamics, but not by either increasing bradykinin activity or reducing blood pressure in this rat model of mesangial proliferative GN.  (+info)

Addition of angiotensin II receptor blockade to maximal angiotensin-converting enzyme inhibition improves exercise capacity in patients with severe congestive heart failure. (4/1416)

BACKGROUND: Incomplete suppression of the renin-angiotensin system during long-term ACE inhibition may contribute to symptomatic deterioration in patients with severe congestive heart failure (CHF). Combined angiotensin II type I (AT1) receptor blockade and ACE inhibition more completely suppresses the activated renin-angiotensin system than either intervention alone in sodium-depleted normal individuals. Whether AT1 receptor blockade with losartan improves exercise capacity in patients with severe CHF already treated with ACE inhibitors is unknown. METHODS AND RESULTS: Thirty-three patients with severe CHF despite treatment with maximally recommended or tolerated doses of ACE inhibitors were randomized 1:1 to receive 50 mg/d losartan or placebo for 6 months in addition to standard therapy in a multicenter, double-blind trial. Peak aerobic capacity (V(O2)) during symptom-limited treadmill exercise and NYHA functional class were determined at baseline and after 3 and 6 months of double-blind therapy. Peak V(O2) at baseline and after 3 and 6 months were 13.5+/-0.6, 15.1+/-1.0, and 15.7+/-1.1 mL. kg-1. min-1, respectively, in patients receiving losartan and 14.1+/-0.6, 14.3+/-0.9, and 13.6+/-1.1 mL. kg-1. min-1, respectively, in patients receiving placebo (P<0.02 for treatment group-by-time interaction). Functional class improved by at least one NYHA class in 9 of 16 patients receiving losartan and 1 of 17 patients receiving placebo. CONCLUSIONS: Losartan enhances peak exercise capacity and alleviates symptoms in patients with CHF who are severely symptomatic despite treatment with maximally recommended or tolerated doses of ACE inhibitors.  (+info)

Angiotensin converting enzyme inhibitors and angiotensin receptor (AT1) antagonists: either or both for primary renal disease? (5/1416)

At the present time we cannot assume that the proven benefits of ACEI on renal disease will be reproduced by using AT1-ra. With potentially differing modes of activity of these drugs, they cannot be seen as interchangeable and ACEI should remain the drug of choice in patients with progressive renal disease unless they are not tolerated. It is possible that AT1-ra may offer additional advantages in some patients or that synergy exists between the two agents, but this view will remain entirely speculative unless proper trials are conducted. Despite the results of the ELITE study [22], the uncertainty regarding the use AT1-ra in cardiovascular disease mirrors that of renal disease. This issue is obviously of relevance to the nephrologist in view of the spectrum of cardiac disease that accompanies chronic renal failure, such as left ventricular hypertrophy and cardiac failure, which provide multiple indications for manipulation of RAS. Despite their renoprotective effect, previous studies on ACEI [3,4] have not shown an overall reduction in mortality and this issue needs to be addressed in addition to renoprotection in studies comparing AT1-ra and ACEI.  (+info)

Effects of AT1 receptor blockade after myocardial infarct on myocardial fibrosis, stiffness, and contractility. (6/1416)

Angiotensin II type 1 (AT1) receptor blockade attenuates myocardial fibrosis after myocardial infarction (MI). However, whether inhibition of fibrosis by AT1 receptor blockade influences myocardial stiffness and contractility is unknown. We measured left ventricular (LV) hemodynamics, papillary muscle function, and myocardial stiffness and fibrosis in rats randomized to losartan or placebo 1 day after MI and treated subsequently for 8 wk. Losartan decreased LV and right ventricular weights as well as mean aortic and LV systolic pressures in sham and MI rats. LV end-diastolic pressure increased after MI and was decreased with losartan. Maximal developed tension and peak rate of tension rise and decline were decreased in MI vs. sham rats. Interstitial fibrosis developed after MI and was prevented in losartan-treated MI rats. The development of abnormal myocardial stiffness after MI was prevented by losartan. After MI, AT1 receptor blockade prevents an abnormal increase in myocardial collagen content. This effect was associated with a normalization of passive myocardial stiffness.  (+info)

Resetting of exaggerated tubuloglomerular feedback activity in acutely volume-expanded young SHR. (7/1416)

One purpose of the present study was to evaluate the ability of 7-wk-old spontaneously hypertensive rats (SHR) to reset tubuloglomerular feedback (TGF) activity in response to acute volume expansion (VE). Second, we evaluated the contribution of ANG II, via its action on AT1 receptors, to TGF control of glomerular function during VE. TGF was assessed by micropuncture methods and proximal tubular stop-flow pressure (SFP) determinations in SHR, Wistar-Kyoto rats (WKY), and Sprague-Dawley rats (SD). During euvolemia SHR exhibited enhanced TGF activity. In the same animals acute VE was achieved by infusion of saline (5 ml. h-1. 100 g body wt-1). VE led to resetting of TGF in all three strains. Maximal SFP responses, elicited by a 30-40 nl/min loop of Henle perfusion rate, decreased from 19 to 12 mmHg in SHR and, on average, from 11 to 5 mmHg in WKY and SD (P < 0.001). Tubular flow rate producing a half-maximal response (turning point) shifted to higher flow rates during VE, from 12 to 14 nl/min in SHR and from 15 to 19 nl/min in WKY. Administration of the AT1 receptor blocker candesartan (0.05 mg/kg iv) during sustained VE decreased TGF-mediated reductions in SFP in SHR and slightly increased the turning point in WKY. Nevertheless, other parameters of TGF activity were unaffected by AT1 receptor blockade. In conclusion, young SHR possess the ability to reset TGF activity in response to VE to a degree similar to compensatory adjustments in WKY. However, TGF remains enhanced in SHR during VE. ANG II and its action on AT1 receptors are in part responsible for the exaggerated SFP responses in young SHR during VE.  (+info)

Renal and hemodynamic effects of losartan in conscious dogs during controlled mechanical ventilation. (8/1416)

In 12 conscious dogs, we investigated whether the angiotensin II-receptor antagonist losartan increases renal sodium excretion and urine volume during controlled mechanical ventilation (CMV) with positive end-expiratory pressure. In four experimental protocols, the dogs were extracellular volume (ECV) expanded (electrolyte solution, 0.5 ml. kg-1. min-1 iv) or not and received losartan (100 micrograms. kg-1. min-1 iv) or not. They breathed spontaneously during the 1st and 4th hour and received CMV with positive end-expiratory pressure (mean airway pressure 20 cmH2O) during the 2nd and 3rd hours. In the expansion group, dogs with losartan excreted approximately 18% more sodium (69 +/- 7 vs. 38 +/- 5 micromol. min-1. kg-1) and 15% more urine during the 2 h of CMV because of a higher glomerular filtration rate (5.3 +/- 0.3 vs. 4.5 +/- 0.2 ml. min-1. kg-1) and the tubular effects of losartan. In the group without expansion, sodium excretion (2.0 +/- 0.6 vs. 2.6 +/- 1.0 micromol. min-1. kg-1) and glomerular filtration rate (3.8 +/- 0.3 vs. 3.8 +/- 0.4 ml. min-1. kg-1) did not change, and urine volume decreased similarly in both groups during CMV. Plasma vasopressin and aldosterone increased in both groups, and plasma renin activity increased from 4.9 +/- 0.7 to 7.8 +/- 1.3 ng ANG I. ml-1. h-1 during CMV in nonexpanded dogs without losartan. Mean arterial pressure decreased by 10 mmHg in nonexpanded dogs with losartan. In conclusion, losartan increases sodium excretion and urine volume during CMV if the ECV is expanded. If the ECV is not expanded, a decrease in mean arterial blood pressure and/or an increase in aldosterone and vasopressin during CMV attenuates the renal effects of losartan.  (+info)

The meta-analysis by Etminan and colleagues addresses an interesting question. Do angiotensin II receptor antagonists, similar to β-blockers, calcium channel blockers, and angiotensin-converting enzyme inhibitors (1, 2), reduce the frequency of headaches in patients with hypertension? The pooled results show a reduction in headache frequency with angiotensin II receptor antagonists. The findings should be interpreted with caution, however, because headache was not the primary outcome in any of the individual studies; the angiotensin II receptor antagonists chosen were not standardized; doses were not equivalent; and the definitions and types of headaches were not specified. Did the patients in these studies have tension headaches, migraine headaches, nasosinus headaches, or cluster headaches? Meta-analysis of secondary study endpoints should be considered hypothesis-generating, and the authors rightly call for a clinical trial to confirm the findings of this meta-analysis. The mechanism of ...
List of elements from ATC C09C: Anti-hypertensive. Angiotensin II receptor antagonists (ARBs, sartans) by level of risk according e-lactancia.org
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Table of Contents: Angiotensin receptor antagonists were developed during the 1970th and 80th. In Germany there are seven labeled substances: losartan, valsartan, eprosartan, irbesartan, candesartan, telmisartan, olmesartan. They are all used for hypertension, some have additional indications like diabetic nephropathy or heart failure. In Europe there is no registration for children and adolescents younger than 18 years. In USA losartan and valsartan are labeled for children 6 years and older with primary hypertension. The most important clinical effects of the angiotensin receptor antagonists are lowering of systolic and diastolic blood pressure, antiproteinuric effects and amelioration of left ventricular hypertrophy. This article explores the efficacy and safety of angiotensin receptor antagonists in children and adolescents by means of a systematic review according to the standards of the Cochrane Collaboration. Beyond that a registry for children and adolescents with renal diseases in ...
36 Consistent with this hypothesis it appears that the beneficial effects of AT2R activation are more pronounced in the FVB/N strain, whereas the C57BL/6 strain seems to be associated with more deleterious effects of AT2R activation. 3). In this context it is important to note that ATBP - also known as ATIP and MTSG, since it was cloned independently by three different groups - mediates antiproliferative effects. 9,46 Interestingly, a high level of PLZF expression was especially observed in the heart by Northern blotting,5 which, considering that PLZF might be regulated depending on the genetic background and the (patho)physiological state, could explain the discrepancies in AT2R function observed in this organ. Csikos T, Balmforth AJ, Grojec M et al. Angiotensin AT2 receptor degradation is prevented by ligand occupation. Biochem Biophys Res Commun 1998; 243:142-7. 7. Zhang J, Pratt RE. The AT2 receptor selectively associates with Gialpha2 and Gialpha3 in the rat fetus. J Biol Chem 1996; ...
Generally, the carrier can be anhydrous or aqueous. It can thus comprise an aqueous phase and/or a fatty phase. Thus, in one preferred embodiment of the present invention, the compositions comprise a fatty phase, in particular made of fatty bodies liquid at 25 °C, such as oils from animal, vegetable, mineral or synthetic origin, either volatile or not, fatty bodies solid at 25 °C such as waxes from animal, vegetable, mineral or synthetic origin; of pasty fatty bodies; of gums; and the mixtures thereof. The volatile oils are generally oils having, at 25 °C, a saturating vapor tension at least equal to 0.5 millibar (50 Pa). Fatty phase components include, but are not restricted to: cyclic volatile silicones having 3 to 8 silicon atoms, preferably 4 to 6, cyclocopolymers of the dimethylsiloxane/methylalkylsiloxane type, linear volatile silicones with 2 to 9 silicon atoms, hydrocarbon volatile oils, such as isoparaffins and, more particularly, isododecane and fluorinated oils, ...
The heart is a beating muscle that pumps blood to the body through a network of arteries. The force of the blood is constantly putting pressure on the...
Diovan (Valsartan) is in a class of medications called angiotensin II receptor antagonists. It works by blocking the action of certain chemicals that tighten the blood vessels, so blood flows more ...
Generic Benicar ™ OLMESARTAN, This medicine is an angiotensin II receptor antagonist used to treat high blood pressure. It may also be used to other conditions as determined by your doctor.
Benicar - Benicar is an angiotensin II receptor antagonist used to treat high blood pressure (hypertension). It keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow.
Benicar - Benicar is an angiotensin II receptor antagonist used to treat high blood pressure (hypertension). It keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow.
This study is a multicenter placebo-controlled double-blind randomized clinical trial. The design scheme is depicted in Figure 1. (see below). At the time of screening, all pentoxifylline-naïve participants must have been receiving angiotensin receptor blockers(ARB) per day for no less than 8 weeks and have stable renal function with serum creatinine elevation , 25% in the preceding 8 weeks. For patients taking maximal dose of angiotensin receptor blockers(ARB) for more than 8 weeks, randomization will be started after recruitment. For patients taking submaximal, fixed dose of angiotensin receptor blockers(ARB)for ≥ 8 weeks, with good BP(blood pressure), i.e., ≤ 130/80 mmHg, randomization can also be started after recruitment. However, for patients taking submaximal dose of angiotensin receptor blockers(ARB) with suboptimal BP, i.e., ?130/80 mmHg, patients can be recruited but will not be randomized until the dose of angiotensin receptor blockers(ARB) has been fixed for ≥ 8 weeks, or a ...
PubMed journal article Beyond ONTARGET: angiotensin-converting enzyme inhibition and angiotensin II receptor blockade in combination, a lesser evil in some? were found in PRIME PubMed. Download Prime PubMed App to iPhone or iPad.
Angiotensin Receptor Blocker Angiotensin receptor blocker such as losartan, candensartan and valsartan are useful in treating patient with congestive heart failure and hypertension. Angiotensin receptor blocker will act by binding and blocking angioten
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BACKGROUND: Few studies have directly compared the renoprotective effects of angiotensin II-receptor blockers and angiotensin-converting-enzyme (ACE) inhibitors in persons with type 2 diabetes. METHODS: In this prospective, multicenter, double-blind, five-year study, we randomly assigned 250 subjects with type 2 diabetes and early nephropathy to receive either the angiotensin II-receptor blocker telmisartan (80 mg daily, in 120 subjects) or the ACE inhibitor enalapril (20 mg daily, in 130 subjects). The primary end point was the change in the glomerular filtration rate (determined by measuring the plasma clearance of iohexol) between the baseline value and the last available value during the five-year treatment period. Secondary end points included the annual changes in the glomerular filtration rate, serum creatinine level, urinary albumin excretion, and blood pressure, the rates of end-stage renal disease and cardiovascular events, and the rate of death from all causes. RESULTS: After five ...
Valsartan and hydrochlorothiazide tablets, USP are a combination of valsartan, an orally active, specific angiotensin II receptor blocker (ARB) acting on the AT 1 receptor subtype, and hydrochlorothiazide, a diuretic. Valsartan, a nonpeptide molecule, is chemically described as N-(1-oxopent...
In this systematic review, we identified a significantly increased risk of hyperkalaemia among people prescribed aliskiren (Rasilez; Novartis Pharmaceuticals, Switzerland) in combination with an ACE inhibitor or angiotensin receptor blocker compared with those prescribed monotherapy using aliskiren, an ACE inhibitor, or angiotensin receptor blocker. This risk was about 50% greater in those prescribed combination therapy than among those receiving ACE inhibitors or angiotensin receptor blocker monotherapy, and was about 70% greater in those prescribed combination therapy than among those receiving aliskiren monotherapy. We found no evidence of a significant difference in the risk of acute kidney injury between the study groups.. To date, no published systematic reviews or meta-analyses have evaluated the safety of combination therapy with aliskiren and ACE inhibitors or angiotensin receptor blockers. Previously published pooled analyses of the safety of aliskiren have provided discordant ...
Angiotensin receptor blockers (ARBs) are medications. They are most often prescribed to treat high blood pressure, but can be used to treat other conditions. This sheet tells you how ARBs work and how to use them effectively.
Angiotensin receptor blockers (ARBs) are medications. They are most often prescribed to treat high blood pressure, but can be used to treat other conditions. This sheet tells you how ARBs work and how to use them effectively.
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Primary Hypothesis:. To evaluate the combination of an angiotensin converting enzyme inhibitor (ACEI) with an angiotensin receptor blocker (ARB) vs. standard treatment with angiotensin receptor blocker on the progression of kidney disease in individuals with Type 2 diabetes and overt nephropathy.. The primary outcome is a composite endpoint of reduction in estimated GFR of 30 ml/min/1.73m*m in individuals with an estimated baseline GFR greater than or equal to 60 ml/min/1.73m*m; reduction in estimated GFR of greater than 50% in individuals with an estimated baseline GFR less than 60 mL/min/1.73m*m; progression to end-stage renal disease (defined as need for dialysis, renal transplant or an eGFR less than 15 ml/min/1.73m*m) or death.. Secondary outcome: a renal composite endpoint, defined as; reduction in estimated GFR of more than 50% (for individuals with a baseline estimated GFR less than 60 ml/min/1.73m*m); reduction in estimated GFR of more than 30 ml/min/1.73m*m (for individuals with a ...
The early blood pressure and hemodynamic effects of the converting enzyme inhibitor (CEI), captopril, were compared in 23 hypertensive patients with those of a specific angiotensin II antagonist (AA), [Sar1, Thr8] A II. AA reduced mean arterial pressure (MAP) greater than 10 mm Hg only in seven of 23 patients vs 15 of 23 who responded to CEI (p less than 0.02). With both drugs, changes in MAP were not associated with significant changes in cardiac output (p greater than 0.10 for both drugs), but correlated with changes in systemic resistance (TPR); r = 0.84, p less than 0.001 for AA and r = 0.71, p less than 0.001 for CEI. Changes in TPR and MAP correlated significantly and inversely with log plasma renin activity in both instances; for AA, r = 0.829 and for CEI, r = -0.737; p less than 0.001 for both. The slopes of the two regression lines were not significantly different but the intercepts were +8.47 mm Hg for AA vs -10.17 mm Hg for CEI (p less than 0.001). This quantitative difference in ...
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Recent studies have revealed significant contributory functions of RAS in the pathophysiology of AD. Activation of RAS in the AD brain was reported by some groups.9-11 These findings support the attractive hypothesis that inhibition of the brain RAS could be a new therapeutic strategy for AD.12 Indeed, a recent study showed that treatment with brain-penetrating ACE inhibitors slowed the rate of cognitive decline in AD patients in comparison with other antihypertensive medication.21 However, some in vitro studies have suggested that ACE could play an important role in the metabolism of Aβ,22,23 demonstrating that ACE degraded Aβ and ACE inhibition increased Aβ levels. On the other hand, as treatment of Tg2576 mice with an ACE inhibitor promoted Aβ deposition,24 treatment with ACE inhibitors might be a risk factor for AD. This effect of ACE inhibition on Aβ metabolism should be carefully considered, especially in relation to long-term treatment with ACE inhibitors. Additional studies are ...
Losartan is an angiotensin II receptor antagonist (sometimes called an ARB blocker). Losartan is used to treat high blood pressure (hypertension) in adults and children who are at least 6 years old. It is also used to lower the risk of stroke in certain people with heart disease. Losartan is also used to slow long-term...
Losartan is an angiotensin II receptor antagonist. Losartan keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow. Losartan is used to treat high blood pressure (hypertension) in adults and children who are at least 6 years old. It is also used to lower the risk of stroke in certain...
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Teva-Telmisartan: Telmisartan belongs to a class of medications known as angiotensin II receptor antagonists. These medications reduce blood pressure by blocking the actions of a chemical (angiotensin II) that causes blood vessels to constrict or tighten. It is used to treat mild to moderate high blood pressure.
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Congestive heart failure medications in development are discussed with focus on LCZ696 a novel heart failure medication from Novartis that has shown promise. LCZ696 is an angiotensin receptor antagonist and neprilysin inhibitor (ARNI).
Posts about Angiotensin-receptor blockade and risk of cancer: meta-analysis of randomised controlled trials written by CWRUmedicine
The Food and Drugs Administration has completed a safety review of angiotensin receptor blockers (ARBs) after they were linked with an increased risk of cancer.. This review of 31 randomised clinical trials involving almost 156,000 participants, of whom 84,461 were treated with an ARB, found no increased risk. The review analysed the data for new cancer cases, cancer-related death, breast cancer, lung cancer and prostate cancer. There was no increase in risk for any of these outcomes.. Action: Clinicians and patients can be reassured by this safety review. It is important to note that the overall evidence still places ARBs are still second line to angiotensin converting enzyme inhibitors (ACEIs). ...
Losartan K Kaken is a medicine available in a number of countries worldwide. A list of US medications equivalent to Losartan K Kaken is available on the Drugs.com website.
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TY - JOUR. T1 - Selective angiotensin II receptor antagonism reduces insulin resistance in obese Zucker rats. AU - Henriksen, Erik J.. AU - Jacob, Stephan. AU - Kinnick, Tyson R.. AU - Teachey, Mary K.. AU - Krekler, Michael. N1 - Copyright: Copyright 2017 Elsevier B.V., All rights reserved.. PY - 2001. Y1 - 2001. N2 - Effects of oral administration of the angiotensin II receptor antagonist (selective AT1-subtype) irbesartan on glucose tolerance and insulin action on skeletal-muscle glucose transport were assessed in the insulin-resistant obese Zucker rat. In the acute study, obese rats received either vehicle (water) or irbesartan 1 hour before the experiment. Although irbesartan had no effect on glucose transport (2-deoxyglucose uptake) in the epitrochlearis muscle, which consists mainly of type IIb fibers, acute angiotensin II receptor antagonism led to a dose-dependent increase in insulin action in the predominantly type I soleus muscle. Irbesartan at 25 and 50 mg/kg induced significant ...
The role of angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) reducing risk of cardiovascular events (CVEs) and preserving kidney function in patients with chronic kidney disease is well-documented. However, the efficacy and safety of these agents in dialysis patients is still a controversial issue. We systematically searched MEDLINE, Embase, Cochrane Library and Wanfang for randomized trials. The relative risk (RR) reductions were calculated with a random-effects model. Major cardiovascular events, changes in GFR and drug-related adverse events were analyzed. Eleven trials included 1856 participants who were receiving dialysis therapy. Compared with placebo or other active agents groups, ARB therapy reduced the risk of heart failure events by 33% (RR 0.67, 95% CI 0.47 to 0.93) with similar decrement in blood pressure in dialysis patients. Indirect comparison suggested that fewer cardiovascular events happened during treatment with ARB (0.77, 0.63 to 0.94). The
TY - JOUR. T1 - Angiotensin-converting enzyme inhibitor or angiotensin receptor blocker use is associated with reduced major adverse cardiovascular events among patients with critical limb ischemia. AU - Armstrong, Ehrin J.. AU - Chen, Debbie C.. AU - Singh, Gagan. AU - Amsterdam, Ezra A. AU - Laird, John R.. PY - 2015/6/5. Y1 - 2015/6/5. N2 - Angiotensin converting enzyme inhibitors (ACEIs) or angiotensin receptor blockers (ARBs) are recommended for secondary prevention in peripheral artery disease, but their effectiveness in patients with critical limb ischemia (CLI) is uncertain. We reviewed 464 patients with CLI who underwent diagnostic angiography or endovascular intervention from 2006-2013 at a multidisciplinary vascular center. ACEI or ARB use was assessed at the time of angiography. Major adverse cardiovascular events (MACE), mortality, and major adverse limb events (MALE) were assessed during three-year follow-up. Propensity weighting was used to adjust for baseline differences between ...
Angiotensin-II receptor antagonists (or blockers) are a newer class of antihypertensive agents. These drugs are selective for angiotensin II (type 1 receptor); unlike angiotensin-converting enzyme inhibitors, they do not inhibit bradykinin metabolism or enhance prostaglandin synthesis. Angiotensin-II receptor antagonists are well tolerated. Cough occurs much less often with these agents than with angiotensin-converting enzyme inhibitors, and they do not adversely affect lipid profiles or cause rebound hypertension after discontinuation. Clinical trials indicate that angiotensin-II receptor antagonists are effective and safe in the treatment of hypertension. Their use in congestive heart failure and renal disease is under investigation.
TY - JOUR. T1 - Clinical and economic implications of therapeutic switching of Angiotensin receptor blockers to Angiotensin-converting enzyme inhibitors. T2 - a population-based study. AU - Kurdi, Amanj. AU - Elliott, Rachel A.. AU - Chen, Li-Chia. PY - 2019/6/1. Y1 - 2019/6/1. N2 - OBJECTIVE: To evaluate the clinical and cost impact of switching angiotensin receptor blockers (ARBs) to angiotensin-converting enzyme inhibitors (ACEIs) in patients with hypertension. METHODS: This study used the UK Clinical Practice Research Datalink, linking with the Hospital Episode Statistics (April 2006 to March 2012). Adults with hypertension (n = 470) were followed from the first ARB prescription date to the switching date (preswitching period); then from the switching date to the date when study ended, patient left the dataset or died (postswitching period). Patients were divided into ACEIs-combined (n = 369) and ACEIs-monotherapy (n = 101) groups by whether additional antihypertensive drugs were prescribed ...
Background; Angiotensin receptor blocker (ARB) is being extensively used to control hypertension. But, there have been limited data whether ARB is associated with increased incidence of new-onset diabetes mellitus (DM) or impaired glucose intolerance (IGT).. Methods; We investigated total 13,561 patients (pts) that was glycerate hemoglobin level , 6.0% and fasting glucose level , 124 mg/dL (ARB therapy group=3421 and control group=9808) from January 2004 to February 2012. To adjust potential confounders, a propensity score matched analysis was performed using the logistic regression model. The primary end-point was the cumulative incidence of new-onset DM, IGT, and impaired fasting glucose (IFG). Also, multivariable cox-regression analysis by adjusted by aforementioned variables was performed to determine the impact of statin therapy on the incidence of new-onset DM, IGT, and IFG.. Results; Mean follow-up duration was 534±604 days in all-pt group, and 608±607 days in propensity score matching ...
TY - JOUR. T1 - Discontinuation of Angiotensin Converting Enzyme Inhibitors and Angiotensin Receptor Blockers in Chronic Kidney Disease. AU - Qiao, Yao. AU - Shin, Jung Im. AU - Sang, Yingying. AU - Inker, Lesley A.. AU - Secora, Alex. AU - Luo, Shengyuan. AU - Coresh, Josef. AU - Alexander, G. Caleb. AU - Jackson, John W.. AU - Chang, Alex R.. AU - Grams, Morgan E.. PY - 2019/11/1. Y1 - 2019/11/1. N2 - Objective: To assess the patterns of angiotensin converting enzyme inhibitors and angiotensin receptor blockers (ACE-I/ARB) discontinuation in the setting of chronic kidney disease (CKD) progression in real-world clinical practice. Patients and Methods: We identified incident ACE-I/ARB users with a baseline estimated glomerular filtration rate (eGFR) ≥15 mL/min/1.73 m2 and without end-stage renal disease in the Geisinger Health System between January 1, 2004, and December 31, 2015. We investigated the associations of CKD stage, hospitalizations with and without acute kidney injury (AKI), serum ...
Animation showing: Physiology of the renin angiotensin aldosteone system (RAAS). Mechanism of action of ACE inhibitors, Angiotensin II receptor blockers (ARBs).
The thesis structure: 148 pages of computer-writing which include: introduction, literature review, materials and methods, 2 chapters with the results of own researches, general conclusions, practical recommendations, bibliography which includes 163 sources, annexes, 33 tables and 42 figures. 12 scientific articles on the basis of the work are published. Domain of application: pharmacology, clinical pharmacology. Aim and objectives: to study the clinical and pharmacological aspects of angiotensin converting enzyme inhibitor lisinopril, angiotensin II receptor antagonist losartan and their combination in the treatment of chronic heart failure of II-IV functional classes. Objectives. determine the evolution of clinical, hemodynamic and morpho-functional parameters of the heart of patients with ischemic CHF during complex treatment with losartan; to assess the efficacy of treatment with lisinopril complex of patients with ischemic CHF after development of clinical symptoms and morpho-functional ...
Quantitative autoradiography was used to characterize angiotensin AT1 and AT2 receptors, in the rat aorta at three developmental ages; embryonic day 18 (E18), and postnatal weeks 2 and 8. The expression of angiotensin receptors was higher in the aorta of E18 and 2-week-old rat. A major proportion of the angiotensin receptors expressed in the aorta at these two ages was AT2 (84 and 81% respectively). Conversely, in the aorta of 8-week-old rats, AT1 was the predominant angiotensin receptor subtype (71%). In 8-week-old rats, the AT2 subtype was also present (28%). In pre- and postnatal rats, [125I]Sar1-angiotensin II binding to AT1 receptors was sensitive to GTP gamma S whereas binding to AT2 receptors was not. AT2 receptors may serve an important role during stages of rapid growth of the aorta, and also have a significant function in the adult vasculature ...
2017 The Author. Published by Oxford University Press for the Infectious Diseases Society of America. Background. Although statins, angiotensin-converting enzyme inhibitors (ACEI) or angiotensin receptor blockers (ARB) are generally well tolerated, the impact of these therapies individually or in combination on the change in neurocognitive function in persons with human immunodeficiency virus infection is unknown. Methods. The study included participants in the AIDS Clinical Trials Group Longitudinal Linked Randomized Trials cohort participants not receiving a statin or ACEI/ARB within 30 days of first neurologic assessment (baseline), with assessments by NPZ-3 (z score of averaged Trailmaking A and B tests and digit symbol test [DST]) from ≥2 measurements. Marginal structural models estimated the causal effect of statin or ACEI/ARB initiation on neurocognitive function; initial constant slope was assumed during the first year of treatment and a second constant slope thereafter. Results. Of ...
Both angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor blockers (ARBs) reduce angiotensin action. Angiotensin, a powerful hormone, has many actions, the most important of which is constriction of small blood vessels, leading to a rise in blood pressure and therefore in the pressure of blood within the glomerular capillaries in the kidneys. Lowering this pressure may well be the mechanism by which these drugs tend to slow progression of kidney failure.. The effects of ACEIs differ from those of ARBs in several important respects. It is even conceivable that taking drugs from both classes is more effective than taking just one or the other alone. Unfortunately, side-to-side comparisons of these two classes of drugs have not been performed, because the drug industry has no interest in such trials. These drugs are also effective in reducing urinary protein excretion in the nephrotic syndrome, and they also slow progression of chronic renal failure even when added to a ...
TY - JOUR. T1 - Angiotensin-Converting Enzyme Inhibitors and Angiotensin Receptor Blockers in Myocardial Infarction. AU - Kostis, John. PY - 2019/7/1. Y1 - 2019/7/1. UR - http://www.scopus.com/inward/record.url?scp=85065221731&partnerID=8YFLogxK. UR - http://www.scopus.com/inward/citedby.url?scp=85065221731&partnerID=8YFLogxK. U2 - https://doi.org/10.1177/1074248419841636. DO - https://doi.org/10.1177/1074248419841636. M3 - Letter. C2 - 31035789. VL - 24. JO - Journal of Cardiovascular Pharmacology and Therapeutics. JF - Journal of Cardiovascular Pharmacology and Therapeutics. SN - 1074-2484. IS - 4. ER - ...
Perhaps the greatest limitation of current pain management is that the tools we have on hand are primarily palliative. While chronic pain can be ameliorated temporarily by interfering with nociceptor signaling pathways or by altering central affective processing, pharmacotherapy has little to offer when it comes to addressing underlying biological processes that lead to the establishment of chronic pain.. That may be about to change. The successful conclusion of the phase 2 clinical trial of the angiotensin II receptor type 2 (AT2) antagonist EMA401 serves as the vanguard for development of a promising new class of analgesics. The study by Rice et al. on behalf of Spinifex Pharmaceuticals shows convincingly that long-term treatment with an AT2 blocker is at least as effective as conventional therapies in ameliorating symptoms of post-herpetic neuralgia. EMA401 also appeared to be free of major side effects, perhaps in part because it does not accumulate in the CNS and therefore presumably ...
The goal of this request was to estimate the number of prevalent users and dispensings of angiotensin-converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs) among pediatric pop
Gratuit Deadspin Up All Night: Here Comes The Heat Thank you for your continued support of Deadspin. Heres hoping your weekend was pleasant. Thank you for your continued support of Deadspin. Heres hoping your ... Index WH WY Select a different Surname Index Select a different Forename Index ... WhaleyBridge.Com Carnival day this year in Whaley Bridge is planned for Saturday 24 June. Plans are still being developed and there is still time to get involved. Real Ghost Stories from California, United States Page 1 ... Real Ghost Stories from California, United States Page 1 Your source for real ghost stories. Submit your paranormal experience! Renoprotective Effect of the Angiotensin Receptor Antagonist Original Article. Renoprotective Effect of the Angiotensin Receptor Antagonist Irbesartan in Patients with Nephropathy Due to Type 2 Diabetes. Edmund J. Lewis, M.D ... whale Weblio whale ( whaleswhale) , () ... Literature Learning Guides Teacher Resources Shmoop Dive into our treasure trove of free ...
Randomised controlled trial of a Calcium Channel or Angiotensin Converting Enzyme Inhibitor/Angiotensin Receptor Blocker Regime to Reduce Blood Pressure Variability following Ischaemic Stroke (CAARBS): a protocol for a feasibility study.
Angiotensin receptor blockers for the reduction of proteinuria in diabetic patients with overt nephropathy: results from the AMADEO study Prasad Bichu1, Ravi Nistala1, Asma Khan2, James R Sowers2, Adam Whaley-Connell11Divisions of Nephrology and Endocrinology; 2Department of Internal Medicine, University of Missouri-Columbia School of Medicine, Columbia Missouri, USAAbstract: Diabetic kidney disease is characterized by persistent albuminuria (>300 mg/dl or >200 μg/min) that is confirmed on at least 2 occasions 3 to 6 months apart, with a progressive decline in the glomerular filtration rate (GFR), elevated arterial blood pressure, and an increased risk for cardiovascular morbidity and mortality. Diabetic kidney disease is the leading cause of end stage renal disease (ESRD) prompting investigators to evaluate mechanisms by which to slow disease progression. One such mechanism is to block the activity of angiotensin II at the receptor site and agents that follow this mechanism are referred to as
Initial studies suggested that angiotensin converting enzyme (ACE) inhibitors, angiotensin receptor blockers (ARBs), and (possibly) aldosterone antagonists might either prevent new onset and recurrent atrial fibrillation (AF) or reduce the rate of ma
Abstract of Paper: Effect Of Angiotensin-II Receptor Blockade On Experimental Portal hypertension In Rabbits , Author: Sherif w. Mansour, Mohamed Abd El Homed and Mohamed Adel El-Sayed * , Year: 2003 , Faculty of Medicine, Benha University
Labeling of rat heart muscarinic receptors using the new M2 selective antagonist [3H]AF-DX 384 Genomics as knowledge enterprise: Implementing an electronic research habitat at the Biopolis Experimental Therapeutics Center Function of the SIRT1 protein deacetylase in cancer Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist A Review on Telmisartan: A Novel, Long-Acting Angiotensin II-Receptor Antagonist Cardioselectivity of AQ-RA 741, a novel tricyclic antimuscarinic drug Angiotensin II receptors in the rat lung are of the AII-1 subtype Production of thrombin at macroscopic surfaces Regulation of Tissue Factor-Mediated Initiation of the Coagulation Cascade by Cell Surface Grp78 Molecular and Cell Biology for Dummies ISBN 0470430664 Cooperation Between VEGF and TNF-a Is Necessary for Exposure of Active Tissue Factor on the Surface of Human Endothelial Cells The technique of measuring thrombin generation with fluorogenic substrates: 1. Necessity of adequate
Losartan is a 4-chloro-5-hydroxymethylimidazole derivative that is a potent and highly selective angiotensin II receptor antagonist. Losartan is metabolized in vivo in rats, monkeys, and humans to a carboxylic acid derivative E3174 that is pharmacologically more active than the parent compound. We have investigated the mechanism of this biotransformation in human liver preparations. The oxidation of both losartan and the putative aldehyde intermediate E3179 was catalyzed by the microsomal fraction, required both NADPH and molecular oxygen, and was inhibited by SKF 525-A, implicating cytochrome P450 (CYP). When incubations with each substrate were performed under an atmosphere of 18O2, the extent of 18O incorporation into the carboxylic acid product was consistent with a mechanism for losartan oxidation involving an aldehyde intermediate. To substantiate the involvement of CYP in these reactions, incubations with losartan and the aldehyde E3179 were performed in the presence of isoform-selective ...
TY - JOUR. T1 - Angiotensin receptor blockers. T2 - Clinical relevance and new opportunities. AU - Volpe, Massimo. PY - 2012. Y1 - 2012. N2 - Effective treatment of high blood pressure (BP) is a key strategy for reducing the burden of hypertension-related cardiovascular diseases, ie, mainly stroke, myocardial infarction, heart failure, and cardiovascular death. Despite these well-established concepts, however, hypertension remains poorly controlled worldwide. In addition, patients treated for hypertension often remain at a higher risk as compared to the normotensive population, even when a satisfactory BP control is achieved. This is due to the concomitant presence of metabolic abnormalities and/or organ damage, thus accounting for the high or very high added cardiovascular risk profile often observed in patients with hypertension. An emerging strategy to improve general BP control and achieve this unmet target for cardiovascular disease prevention in patients with hypertension is represented by ...
It is well-known that cardiac hypertrophy and arterial and renal dysfunction are serious complications of hypertension. Therefore, we investigated the chronic effects of 606A (2-propyl-3-[2′(1,I,H,/I,-tetrazole-5-yl)biphenyl-4-yl]methyl-5-acetyl-4, 5, 6, 7-tetrahydro imidazo[4, 5-,I,c,/I,]pyridine-4-carboxylic acid disodium salt), a novel AT,SUB,1,/SUB,-receptor antagonist, on these complications of hypertension in stroke-prone spontaneously hypertensive rats (SHRSP) using Wistar Kyoto rats (WKY) as the control. After 8 weeks treatment from 16 weeks of age with 606A by a subcutaneously implanted osmotic pump, cardiac function, cardiac weight, acetylcholine-induced endothelium-dependent relaxation in the isolated aorta and renal function were estimated. Furthermore, wall thickness of the left ventricle was studied morphologically. We found that 606A (0.3 mg, 1 mg and 3 mg/head/day) dose-dependently lowered blood pressure without any effects on heart rate in SHRSP. Long-term treatments with 606A ...
Renin-angiotensin system inhibitors, specifically angiotensin II converting enzyme inhibitors (ACEI) and angiotensin II receptor blockers (ARB), have confirmed renoprotective benefits in patients with proteinuria and hypertension. However, it remains controversial whether these agents are beneficial to kidney recipients. We conducted this meta-analysis to evaluate the effects of ACEI/ARB treatment on patient and allograft survival after kidney transplant. The PubMed, Embase and Cochrane Library databases were searched for eligible articles from before May 2016, and we included 24 articles (9 randomised controlled trials [RCTs] and 15 cohort studies with 54,096 patients), in which patient or graft survival was compared between an ACEI/ARB treatment arm and a control arm ...
Ibresartan is available in 75, 150 and 300 mg tablets generically and under the trade name Avapro. 5mg/150mg and 12. Avalide If you think of using the irbesartan , remember it is a blood pressure medication. Buy Tetracycline Topical Irbesartan is an angiotensin II receptor antagonist which works by relaxing …. 5 mg of hydrochlorothiazide. The catalog displays all strengths and sizes along with the description, imprint code, NDC and …. Contrary to Sanderss assertions, the intrinsic-value test 2 for taxable sales is simply a variant of the investment-theory test advanced by the state at trial Videos in the series are filmed inside two Airstream trailers at Bottletree, avalide tab 150mg an Avondale concert venue. It belongs to a class of drugs called angiotensin receptor blockers ( Avalide Tab 150mg ARBs ) which also includes valsartan ( Diovan ), losartan ( Cozaar ), and candesartan ( Atacand ) Irbesartan is the generic form of the brand-name drug Avapro, which is used to treat high blood ...
Patients with type 2 diabetes frequently have to be treated with more than one drug. Effects of oral antidiabetic drugs depend on the extent of drug absorption from the gut lumen, on metabolism of the drug in the liver, and on the extent of its excretion into bile and urine (21). In general, modification of all these processes by a second, concomitantly administered drug can alter the effects of oral antidiabetic drugs (21).. Recently, it was recognized that a broad variety of drugs, including many cardiovascular drugs such as statins and angiotensin II-receptor antagonists, is transported through biological membranes via specific transport proteins (15,22-24). For example, the efflux transporter P-glycoprotein, which translocates its substrates from the inside of the cell to the outside (e.g., from the hepatocyte into bile) is a major determinant of drug effects (1). If P-glycoprotein-mediated drug excretion is inhibited by a second, concomitantly administered compound, drug plasma ...
Abstract:. Candesartan is potent antihypertensive drug of class angiotensin II receptor antagonist. But it exhibits poor water solubility and extensive first pass metabolism. Present research deals with development of candesartan buccal film. Optimisation of buccal film was done by design expert. Optimised concentration range selected for development of trial batches of candesaratanbuccal films. Mucoadhesivebuccal films of candesartan were prepared by solvent casting technique using chitosan, HPMC, gelatin and EDTA as permeation enhancer. Prepared buccal films evaluated for various pharmaceutical parameters, stability studies, in-vitro and ex-vivo evaluation parameters performed. In-vitroangiotensin II receptor antagonist studies were also performed. Results showed improved bioavaibility of candesartan through buccal films.. ...
Supplementary Materials Supplemental file 1 IAI. IL-12 creation in neutrophils, accompanied by IRF-1 and AP-1 gene expression. Bacteria in which the exported repetitive protein (Erp)-like gene was deleted ([2,C5], get away from phagosomes by [2, 6, 7] and [2, 8, 9], and reprogramming of phagosome maturation by [2, 10,C12]). Such bacterial persistence can result in chronic, latent, or low-grade attacks in the sponsor (13,C15). A number of chemical agents have already been developed to take care of persistent bacterial attacks in mammals. In the entire case of LY2801653 (Merestinib) bacterial attacks recalcitrant to chemical substance treatment, however, vaccines are used like a preventive measure often. Live-attenuated vaccines, like the bacillus Calmette-Gurin (BCG) vaccine, work against these diseases often. In some full cases, authorized inactivated vaccines show poor effectiveness (16, 17) because they dont induce solid cell-mediated immunity (CMI), which straight kills contaminated cells ...
The guidelines above are for the general population, but seniors health needs and benchmarks differ from those of younger individuals in many ways. While 130/80 mmHg is the generic threshold for beginning BP medications, there have been many disagreements among medical professionals regarding the threshold for older adults. Age, frailty and other comorbidities like diabetes and chronic kidney disease complicate this matter even further.. The Eighth Joint National Committee (JNC 8) issued guidelines in 2013 recommending that individuals over age 60 aim for a reading below 150/90 mmHg. The JNC 8 recommendation for patients of any age with diabetes or chronic kidney disease is to aim for BP readings below 140/90 mmHg. These are not hard and fast rules, though, because each seniors health needs are unique.. The JNC 8 guidelines support what we geriatricians have believed for quite some time: many older adults are taking too much BP medication, says Dr. Leslie Kernisan, M.D., M.P.H. In addition ...
The angiotensin receptors are seven-membrane G-protein-coupled receptors. They mediate the cardiovascular and other effects of angiotensin II which is a bioactive peptide of the renin-angiotensin system.. ...
Cozaar (losartan) can be used in combination with other medications to treat high blood pressure. Only a qualified health care professional can make such a decision - to combine this medication with other drugs for best effects. This medicine belongs to the class of angiotensin II receptor antagonists and provides for a better blood flow.
benicar side effects medication. Benicar is used for treating high blood pressure, alone or with other medicines. It may also be used for other conditions.. benicar savings card. Do not take double dose. If you miss a dose you should take it as soon as you remember about your missing. If it is the time for the next dose you should continue your regular dosing schedule.. benicar generic version. If you overdose Benicar and you dont feel good you should visit your doctor or health care provider immediately.. how much does benicar 20 mg cost. Store your medicine at room temperature between 15 and 30 degrees C (59 and 86 degrees F) away from moisture and heat. Throw away any unused medicine after the expiration date. Keep out of the reach of children and in a container that small children cannot open.. benicar hct uses. Benicar is an angiotensin II receptor antagonist. It works by inhibiting the action of a chemical transmitter (angiotensin II) and allowing the blood vessels to dilate (widen) and ...
Cozaar is in a group of drugs called angiotensin II receptor antagonists. It keeps blood vessels from narrowing, which lowers blood pressure and improves blood flow. Cozaar is used to treat high blood pressure (hypertension). It is also used to lower the risk of stroke in certain people with heart disease. It is used to slow long-term kidney damage in people with type 2 diabetes who also have high blood pressure and protein in the urine (proteinuria). It may be used alone or in combination with a diuretic ...
Cheng J, Zhang W, Zhang X, et al. Effect of angiotensin-converting enzyme inhibitors and angiotensin II receptor blockers on all-cause mortality, cardiovascular deaths, and cardiovascular events in patients with diabetes mellitus: a meta-analysis. JAMA Intern Med. 2014;174:773-85. 24687000 ...
Olvance Contain Olmesartan as active ingredient. It belong to the group of drug called angiotensin II receptor antagonists.Olmesartan keep blood vessel from narrowing & lower blood pressure and improve blood flow.
Information about this combination antihypertension medication, including a diuretic and an angiotensin II receptor antagonist, used to treat hypertension or high blood pressure. ...
Results We identified 100 043 patients with a first-time stroke. Of these, 83 736 patients had ischaemic stroke, 11 779 had ICH, and 4528 had SAH. For ischaemic stroke, the adjusted 30-day MRR was reduced in current users compared with non-users (0.85, 95% CI 0.81 to 0.89). There was no reduction in the adjusted 30-day MRR for ICH (0.95, 95% CI 0.87 to 1.03) or SAH (1.01, 95% CI 0.84 to 1.21), comparing current users with non-users. No association with mortality was found among former users compared with non-users. No notable modification of the association was observed within sex or age strata. ...
Buy Telmisartan (CAS 144701-48-4), a selective angiotensin II (AT1) antagonist. Join researchers using high quality Telmisartan from Abcam and achieve your…
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Patients with underlying cardiovascular diseases appear to have an increased risk for adverse outcomes with coronavirus disease 2019 (COVID-19). Although the clinical manifestations of COVID-19 are dominated by respiratory symptoms, some patients also may have severe cardiovascular damage. Angiotensin converting enzyme 2 (ACE2) receptors have been shown to be the entry point into human cells for SARS-CoV-2, the virus that causes COVID-19. In a few experimental studies with animal models, both angiotensin converting enzyme (ACE) inhibitors and angiotensin receptor blockers (ARBs) have been shown to upregulate ACE2 expression in the heart. Though these have not been shown in human studies, or in the setting of COVID-19, such potential upregulation of ACE2 by ACE inhibitors or ARBs has resulted in a speculation of potential increased risk for COVID-19 infection in patients with background treatment of these medications.. ACE2 is a homolog of angiotensin converting enzyme (ACE). ACE2 negatively ...
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Previous studies have also linked hypertension to severe coronavirus disease (COVID-19). Now, a new study by researchers at the University of East Anglias Norwich Medical School has found that the risk of severe COVID-19 and death was reduced for patients with high blood pressure who were taking Angiotensin-Converting Enzyme inhibitors (ACEi) or Angiotensin Receptor Blockers (ARB).. ...
You have mild CKD insofar as your GFR is concerned. Regarding the protein levels in your urine, could you kindly post the units of both measurements as each lab uses different expressions for albuminuria and creatinine around the world, and I want to be sure what we are referring to. If your urinary protein is elevated, but only mildly so, then again, this would fall under the mild CKD category. The priority moving forward would be maintaining a blood pressure of less than 140/90 as an absolute maximum and some authorities would recommend even lower, 130/80. As well, it would be important to maintain urinary proteins in a low range with adequate BP control and possible use of ACE inhibitors or Angiotensin Receptor blockers. Once I know the precise urinary protein measurements, I will have a better handle on the degree to which this is the case at present ...
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... , otherwise known as the compound SC-52458, is a nonpeptide angiotensin II receptor antagonist (ARB, AT1 receptor ... an orally active angiotensin II-receptor antagonist: inhibition of blood pressure response to angiotensin II challenges and ... Usune S, Furukawa T (October 1996). "Effects of SC-52458, a new nonpeptide angiotensin II receptor antagonist, on increase in ... October 1993). "Pharmacology of SC-52458, an orally active, nonpeptide angiotensin AT1 receptor antagonist". Journal of ...
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As with other angiotensin II receptor antagonists, candesartan is indicated for the treatment of hypertension. Candesartan has ... Jul-Aug 1993). "Pilot study of a new angiotensin II receptor antagonist, TCV-116: effects of a single oral dose on blood ... 1992). "Hypotensive activity of TCV-116, a newly developed angiotensin II receptor antagonist, in spontaneously hypertensive ... Anemia may occur, due to inhibition of the renin-angiotensin system. As with other angiotensin receptor blockers, candesartan ...
Sever, P. S.; Hughes, A. (June 2001). "Angiotensin receptor antagonists and vaso-vagal attacks due to sensitisation of the ... angiotensin II type 1 receptor (AT1) antagonists and serotonin agonists. It may also contribute to various pathophysiological ... The pathway for this cardioprotective reflex begins with receptors in the ventricles of the heart, which detect mechanical and ... The myelinated afferents originating in the atria are attached to discrete receptor endings, whereas most of the unmyelinated ...
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It is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II. Telmisartan was patented in ... Telmisartan is an angiotensin II receptor blocker that shows high affinity for the angiotensin II receptor type 1 (AT1), with a ... Side effects are similar to other angiotensin II receptor antagonists and include tachycardia and bradycardia (fast or slow ... May 2004). "Identification of telmisartan as a unique angiotensin II receptor antagonist with selective PPARgamma-modulating ...
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Hence MAS1 receptor agonists have similar therapeutic effects as angiotensin-II receptor antagonists including lowering blood ... The MAS1 oncogene (MAS receptor) is a G protein-coupled receptor, which binds the angiotensin-II metabolite Angiotensin (1-7). ... The MAS1 receptor when activated by binding angiotensin-(1-7) opposes many of the effects of angiotensin-II activated ... "Physical Exercise and ACE2-Angiotensin-(1-7)-Mas Receptor Axis of the Renin Angiotensin System". Protein and Peptide Letters. ...
Angiotensin II receptor antagonists (ARBs) block the angiotensin II receptors that are linked to hypertension and heart failure ... ACE inhibitors works upstream from angiotensin II receptor antagonists and have similar effects on management of hypertension ... The adrenergic receptor is a set of receptors that are commonly manipulated. Four properties of the heart - chronotropy, ... that manipulate the adrenergic receptors and have variable specificity for the receptors and are, thus, used for various ...
Ip S, Tsang S, Wong T, Che C, Leung P (2003). "Saralasin, a nonspecific angiotensin II receptor antagonist, attenuates ... Saralasin is a partial agonist of angiotensin II receptors, though it is commonly mistaken as a competitive antagonist. ... In other words, the effects of saralasin on the angiotensin II receptor in the absence of angiotensin II is pharmacodynamically ... because if it was an antagonist it would not elicit an effect when bound to its receptor. Saralasin is an angiotensin II ...
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For instance, a receptor antagonist is an agent that reduces the response that a ligand produces when the receptor antagonist ... For example, not only do angiotensin receptor blockers, and angiotensin-converting enzyme (ACE) inhibitors work to lower blood ... An example of this is the interleukin-1 receptor antagonist. The opposite of antagonism is synergy. It is a negative type of ... Kalaitzidis, R; Bakris, G. L. (2009). "Effects of angiotensin II receptor blockers on diabetic nephropathy". Journal of ...
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... beta-adrenoreceptor antagonists, angiotensin-converting enzyme inhibitors and angiotensin-2 receptor blockers. Doxazosin is ... Like other alpha-1 receptor antagonists, it has a role in the peri-operative management of pheochromocytoma. Doxazosin is ... Doxazosin is usually added to other antihypertensive therapy such as calcium channel antagonists, diuretics, ... "Time to re-appraise the role of alpha-1 adrenoceptor antagonists in the management of hypertension?". Journal of Hypertension. ...
... role of type I angiotensin II receptor antagonist". Translational Research. 165 (5): 599-620. doi:10.1016/j.trsl.2014.11.005. ... "Angiotensin II and myosin light-chain phosphorylation contribute to the stretch-induced slow force response in human atrial ...
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Fimasartan is a non-peptide angiotensin II receptor antagonist developed by Boryung Pharmaceutical to treat hypertension and ...
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Cannabinoid receptor antagonists. *CCR5 receptor antagonists. *Neurokinin 1 receptor antagonists. *5-HT3 antagonists ... The GABAA receptors are made up of subunits which form a receptor complex. Humans have 19 receptor subunits and are classified ... See also: Receptor/signaling modulators • GABA receptor modulators • GABA metabolism/transport modulators ... and sigma receptors.[18] The neurosteroid Progesterone (PROG) that activates progesterone receptors expressed in peripheral and ...
Antagonist: A drug with a fast association & slow dissociation. Induced-fitEdit. As a drug approaches a receptor, the receptor ... Boulay G, Chrétien L, Richard DE, Guillemette G (November 1994). "Short-term desensitization of the angiotensin II receptor of ... GABA receptors: GABA-A, GABA-C. GABA. Cl− , HCO−3 [11]. Glutamate receptors: NMDA receptor, AMPA receptor, and Kainate receptor ... toll-like receptors (TLRs), killer activated and killer inhibitor receptors (KARs and KIRs), complement receptors, Fc receptors ...
transmembrane signaling receptor activity. • Wnt-activated receptor activity. • G-protein coupled receptor activity. ... "Purification and molecular cloning of a secreted, Frizzled-related antagonist of Wnt action". Proc. Natl. Acad. Sci. U.S.A. 94 ... "Frizzled Receptors: FZD5". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it.. *v ...
receptor 2 antagonists amphotericin B, lithium[13][14]. Inhibits vasopressin's action 5. collecting duct ... Ballew JR, Fink GD (September 2001). "Characterization of the antihypertensive effect of a thiazide diuretic in angiotensin II- ... Aldosterone antagonists: spironolactone, which is a competitive antagonist of aldosterone. Aldosterone normally adds sodium ... a Selective Oral Vasopressin V2-Receptor Antagonist, for Hyponatremia". New England Journal of Medicine. 355 (20): 2099-2112. ...
... and alpha-2 adrenoceptor antagonist activity.[5] D1 receptor stimulation activates adenylyl cyclase and raises intracellular ... The renal effect of fenoldopam and dopamine may involve physiological antagonism of the renin-angiotensin system in the kidney. ... Fenoldopam mesylate (Corlopam) is a drug and synthetic benzazepine derivative which acts as a selective D1 receptor partial ... Grenader A, Healy DP (July 1991). "Fenoldopam is a partial agonist at dopamine-1 (DA1) receptors in LLC-PK1 cells". J. ...
ACE inhibitors, angiotensin receptor blockers, direct renin inhibitors and aldosterone antagonists, are pharmacological ...
... in which case angiotensin II receptor antagonists (ARBs) are the next line of treatment. ... Receptors[edit]. Main article: Bradykinin receptor. *The B1 receptor (also called bradykinin receptor B1) is expressed only as ... The kinin B1 and B2 receptors belong to G protein coupled receptor (GPCR) family. ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ...
Affecting blood pressure/(antihypertensive drugs): ACE inhibitors, angiotensin receptor blockers, beta-blockers, α blockers, ... H2-receptor antagonists, cytoprotectants, prostaglandin analogues. *Lower digestive tract: laxatives, antispasmodics, ... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... Leukotriene antagonists For endocrine problemsEdit. androgens, antiandrogens, estrogens, gonadotropin, corticosteroids, human ...
... also called the cation-independent mannose 6-phosphate receptor), which acts as a signalling antagonist; that is, to prevent ... IGF-2 exerts its effects by binding to the IGF-1 receptor and to the short isoform of the insulin receptor (IR-A or exon 11-).[ ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... insulin receptor binding. • hormone activity. • GO:0001948 protein binding. • growth factor activity. • insulin-like growth ...
renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... NK1 receptor antagonist *Aprepitant (Emend) is a commercially available NK1 Receptor antagonist ... 5-HT3 receptor antagonists block serotonin receptors in the central nervous system and gastrointestinal tract. As such, they ... chemotherapy as a single drug as well as with other antiemetics such as 5-HT3 receptor antagonists and NK1 receptor antagonist ...
It is a peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. ... "Randomized Trial of Icatibant for Angiotensin-Converting Enzyme Inhibitor-Induced Upper Airway Angioedema". The Journal of ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ...
However, Angiotensin converting enzyme inhibitors and Angiotensin II receptor antagonists are favoured due to their anti- ... Importantly, angiotensin-converting enzyme inhibitors were used in both groups equally. Cyclophosphamide ( traded as endoxan & ...
Watts, K; Chavasse, RJ (2012 May 16). "Leukotriene receptor antagonists in addition to usual care for acute asthma in adults ... dan inhibitor enzim pengubah angiotensin.[60] ... "Antianginal actions of beta-adrenoceptor antagonists". Am J ...
Angiotensin II receptor antagonist. *ACE inhibitor. *Alpha-adrenergic agonist. *Beta blocker. *Dopamine agonist ... For receptors, these activities include agonist, antagonist, inverse agonist, or modulator. Enzyme target mechanisms include ...
The ACTH receptor is a seven-membrane-spanning G protein-coupled receptor.[7] Upon ligand binding, the receptor undergoes ... A family of related receptors mediates the actions of these hormones, the MCR, or melanocortin receptor family. These are ... ACTH receptors outside the adrenal gland[edit]. As indicated above, ACTH is a cleavage product of the pro-hormone, ... MC2R is the ACTH receptor. While it has a crucial function in regulating the adrenal, it is also expressed elsewhere in the ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ...
... an angiotensin II receptor antagonist Propranolol, a sympatholytic beta blocker Vasopressin receptor antagonists, such as ... and the effects of an adjunctive angiotensin-II receptor blocking drug (irbesartan)". The Australian and New Zealand Journal of ...
Adenosine receptors Receptor. Gene. Mechanism [15]. Effects. Agonists. Antagonists A1 ADORA1. Gi/o → cAMP↑/↓ *Inhibition *↓ ... The adenosine receptors (or P1 receptors[1]) are a class of purinergic G protein-coupled receptors with adenosine as the ... A2A adenosine receptor[edit]. Main article: Adenosine A2A receptor. As with the A1, the A2A receptors are believed to play a ... The adenosine receptors are commonly known for their antagonists caffeine and theophylline, whose action on the receptors ...
Kalindjian SB, McDonald IM (2007). "Strategies for the design of non-peptide CCK2 receptor agonist and antagonist ligand". ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ... Léna I, Dh tel H, Garbay C, Daugé V (January 2001). "Involvement of D2 dopamine receptors in the opposing effects of two CCK-B ...
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renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... Partial agonist at the mu opioid receptor; agonist at delta opioid receptor; antagonist at kappa opioid receptor.. Sublingual, ... Full agonist at kappa opioid receptors, partial agonist/antagonist at the mu opioid receptors.[39]. IM, IV, SC.. Protein ... Kappa opioid receptor agonist; mu opioid receptor antagonist/partial agonist.. IM, IV, SC.. Bioavailability = 60-70%; protein ...
renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... but other drugs such as CB1 receptor antagonists exist in this class too.[25][26] Drugs used to treat sleep disorders such as ... as well as inhibit the inhibitory effect of adenosine receptors on dopamine receptors,[67] however the implications for humans ... Kamiya T, Saitoh O, Yoshioka K, Nakata H (June 2003). "Oligomerization of adenosine A2A and dopamine D2 receptors in living ...
renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... Active targeting uses biological molecules (antibodies, proteins, DNA and receptor ligands) to preferentially target the ... especially those associated with receptor tyrosine kinases) is known as targeted therapy. ...
renin-angiotensin system *ACE inhibitors. *Angiotensin II receptor antagonists. *Renin inhibitors. *Antihyperlipidemics * ... α-Adrenergic receptor agonists[edit]. Main article: α-Adrenergic receptor agonist. Common or widely marketed[edit]. * ... Pseudoephedrine acts indirectly on the adrenergic receptor system, whereas phenylephrine and oxymetazoline are direct agonists ... α1-adrenergic receptor since they mediate vasoconstriction and constricting nasal vasculature causes decongestion of nasal ...
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"Prostanoid Receptors: EP3". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical ... prostaglandin receptor activity. • signal transducer activity. • prostaglandin E receptor activity. • protein binding. ... Prostaglandin E2 receptor 4 (EP4). അവലംബം[തിരുത്തുക]. *↑ 1.0 1.1 1.2 GRCh38: Ensembl release 89: ENSG00000050628 - Ensembl, May ... "EP3-2 receptor mRNA expression is reduced and EP3-6 receptor mRNA expression is increased in gravid human myometrium". Journal ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Galanin receptor 1 (GAL1) is a G-protein coupled receptor encoded by the GALR1 gene.[5] ... "Galanin Receptors: GAL1". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology ... This transmembrane receptor-related article is a stub. You can help Wikipedia by expanding it. *v ...
... the RAS is targeted pharmacologically by ACE inhibitors and angiotensin II receptor antagonists, also known as angiotensin ... Angiotensin I flows in the bloodstream until it reaches the capillaries of the lungs where angiotensin converting enzyme (ACE) ... acts on it to convert it into angiotensin II.. *Angiotensin II is a vasoconstrictor which will increase blood flow to the heart ... Baroreceptors in low pressure receptor zones (mainly in the venae cavae and the pulmonary veins, and in the atria) result in ...
D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ... Vincent JP (October 1995). "Neurotensin receptors: binding properties, transduction pathways, and structure". Cellular and ... Angiotensin. *Bombesin. *Calcitonin gene-related peptide. *Carnosine. *Cocaine- and amphetamine-regulated transcript ...
... "angiotensin II receptor antagonists" may be prescribed. By attaching to AT1 receptors on smooth muscle cells lining the blood ... The end result is that angiotensin II receptor antagonists prevent blood vessels from narrowing, thereby keeping a normal blood ... There are several different brands of angiotensin II receptor antagonists. As with all medications, adverse effects may develop ... In order to cause vessel narrowing, angiotensin II binds to proteins, called AT1 receptors, on the surface of smooth muscles ...
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Do angiotensin II receptor antagonists, similar to β-blockers, calcium channel blockers, and angiotensin-converting enzyme ... Angiotensin II receptor antagonists vs placebo for preventing headache*. Outcome. Weighted event rates. RRR (95% CI). NNT (CI) ... Review: Angiotensin II receptor antagonists prevent headache in patients with mild-to-moderate hypertension PDF. ACP J Club. ... I will use angiotensin II receptor antagonists as needed for hypertension control and hope that the hypothesis of this study is ...
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Angiotensin II receptors and angiotensin II receptor antagonists. Pharmacol Rev. 1993; 25 : 205 -251. ... Effects of AT1 and AT2 Angiotensin Receptor Antagonists in Angiotensin II-Infused Rats. Jin S. Li, Rhian M. Touyz, Ernesto L. ... Angiotensin II receptor subtypes and growth. In Saavedra JM, Timmermans PBMWM, eds. Angiotensin/Receptors. New York: Plenum ... Effects of AT1 and AT2 Angiotensin Receptor Antagonists in Angiotensin II-Infused Rats ...
Angiotensin II Receptor Antagonists. Class Summary. ARBs interfere with the binding of formed angiotensin II to its endogenous ... Vasopressin Antagonists. Class Summary. The selective vasopressin V2-receptor antagonist, tolvaptan, causes an increase in ... Valsartan is a prodrug that produces direct antagonism of angiotensin II receptors. It displaces angiotensin II from the AT1 ... Tolvaptan (Jynarque), a selective vasopressin V2-receptor antagonist, was approved by the US.Food and Drug Administration (FDA ...
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From the Ninewells Hospital and Medical School, University of Dundee, Dundee, and the *University Department of Medicine and Therapeutics, Western Infirmary, University of Glasgow, Glasgow, UK.. ...
Recent trials have now shown that treatment with beta-blockers, aldosterone antagonists and angiotensin receptor blockers also ... Practical recommendations for the use of ACE inhibitors, beta-blockers, aldosterone antagonists and angiotensin receptor ... Adrenergic beta-Antagonists/therapeutic use*. *Angiotensin Receptor Antagonists*. *Angiotensin-Converting Enzyme Inhibitors/ ...
... non-peptide Angiotensin II (AT1specific) antagonist. It is a new and promising antihypertesive agent, better than ACE in.. ... Angiotensin Receptor Antagonists A New Class Of Antihypertensive Drugs. Author(s): Zeenat S Hakim, Milan C Satia, Ramesh K ... Among other angiotensin receptor antagonists are TCV- 116, CV-11974, and CV-11194, all of which seem to be promising ... Results of the studies on losartan and other angiotensin receptor antagonists indicate that they would certainly acquire a ...
P. A. Datar, P. V. Desai, and E. C. Coutinho, "A 3D-QSAR of angiotensin II (AT1) receptor antagonists based on receptor surface ... M. C. Sharma and D. V. Kohli, "3D-QSAR studies of some substituted imidazolinones angiotensin II receptor antagonists," World ... A. Parate and S. C. Chaturvedi, "Predicting 3H-1,2,4-triazolinones as angiotensin II receptor antagonists: 2D and 3D QSAR by ... M. C. Sharma and D. V. Kohli, "3D QSAR approach on substituted isoxazolidines derivatives as angiotensin II receptor antagonist ...
... angiotensin II receptor blockers, beta-blockers, aldosterone antagonists, cardiac glycosides, diuretics, nitrates, vasodilators ... Angiotensin II Receptor Blockers (ARBs). Class Summary. Angiotensin receptor blockers are as effective as ACE inhibitors in the ... blocks the vasoconstrictor effects of angiotensin II by selectively blocking binding of angiotensin II to the AT-1 receptor in ... Enalapril prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in increased levels of ...
Angiotensin Receptor Antagonists. Antihypertensive Agents. Angiotensin II Type 1 Receptor Blockers. Molecular Mechanisms of ... Effects of Angiotensin Receptor Antagonist on Prohibiting Cardiovascular Events on Hemodialysis Patients. The safety and ... Although angiotensin receptor blockers (ARBs) are effective for patients with diabetes and chronic kidney disease in reducing ... Suzuki H, Kanno Y, Sugahara S, Ikeda N, Shoda J, Takenaka T, Inoue T, Araki R. Effect of angiotensin receptor blockers on ...
Angiotensin II Type 1 Receptor Antagonists and their Combinations in the Treatment of Hypertension ... HypertensionArterial PressurePhenotypeReceptor ; Angiotensin ; Type 1Antihypertensive Agents Abstract: The pathophysiology of ...
ACE Inhibitor or Angiotensin II Receptor Antagonist Attenuates Diabetic Neuropathy in Streptozotocin-Induced Diabetic Rats. ... ACE Inhibitor or Angiotensin II Receptor Antagonist Attenuates Diabetic Neuropathy in Streptozotocin-Induced Diabetic Rats ... ACE Inhibitor or Angiotensin II Receptor Antagonist Attenuates Diabetic Neuropathy in Streptozotocin-Induced Diabetic Rats ... ACE Inhibitor or Angiotensin II Receptor Antagonist Attenuates Diabetic Neuropathy in Streptozotocin-Induced Diabetic Rats ...
Effects of angiotensin-converting enzyme inhibitors and angiotensin II type 1 receptor antagonists in rats with heart failure: ... The beneficial effects of ACE inhibitors (ACEi) or angiotensin II type 1 receptor antagonists (AT1-ant) are reportedly mediated ... Effect of ACE Inhibitors and Angiotensin II Type 1 Receptor Antagonists on Endothelial NO Synthase Knockout Mice With Heart ... Effect of ACE Inhibitors and Angiotensin II Type 1 Receptor Antagonists on Endothelial NO Synthase Knockout Mice With Heart ...
Angiotensin-converting enzyme inhibitors and angiotensin IIâ€"receptor antagonists are recommended for patients with chronic ... Current Guidelines for Using Angiotensin-Converting Enzyme Inhibitors and Angiotensin II-Receptor Antagonists in Chronic Kidney ... Current Guidelines for Using Angiotensin-Converting Enzyme Inhibitors and Angiotensin II-Receptor Antagonists in Chronic Kidney ... The authors found that current guidelines for the use of angiotensin-converting enzyme inhibitors and angiotensin IIâ€"receptor ...
Interaction of nonpeptide angiotensin II receptor antagonists with the urate transporter in rat renal brush-border membranes.. ... Interaction of nonpeptide angiotensin II receptor antagonists with the urate transporter in rat renal brush-border membranes.. ... Interaction of nonpeptide angiotensin II receptor antagonists with the urate transporter in rat renal brush-border membranes.. ... Interaction of nonpeptide angiotensin II receptor antagonists with the urate transporter in rat renal brush-border membranes. ...
To examine whether the response to the angiotensin II receptor antagonist losartan varies depending on the angiotensin ... Angiotensin converting enzyme genotype influences the response to the angiotensin II receptor antagonist losartan in patients ... To examine whether the response to the angiotensin II receptor antagonist losartan varies depending on the angiotensin ... 0/Antihypertensive Agents; 0/Receptors, Angiotensin; 114798-26-4/Losartan; EC 3.4.15.1/Peptidyl-Dipeptidase A ...
Effects of losartan, a nonpeptide angiotensin II receptor antagonist, on cardiac hypertrophy and the tissue angiotensin II ... Significance of angiotensin II receptor blockers with high affinity to angiotensin II type 1 receptors for vascular protection ... A Novel Angiotensin II-Receptor Antagonist, 606A, Induces Regression of Cardiac Hypertrophy, Augments Endothelium-Dependent ... Proximal nephron and renal effects of DuP753, a nonpeptide angiotensin II receptor antagonist XIE MH. ...
Candesartan, an Angiotensin II Receptor Antagonist, Suppresses Pancreatic Inflammation and Fibrosis in Rats. Tamaki Yamada, ... Candesartan, an Angiotensin II Receptor Antagonist, Suppresses Pancreatic Inflammation and Fibrosis in Rats. Tamaki Yamada, ... Candesartan, an Angiotensin II Receptor Antagonist, Suppresses Pancreatic Inflammation and Fibrosis in Rats. Tamaki Yamada, ... Candesartan, an Angiotensin II Receptor Antagonist, Suppresses Pancreatic Inflammation and Fibrosis in Rats ...
Antagonist activity at rat AT1 receptor expressed in CHO cells assessed as angiotensin 2-evoked increase in intracellular ...
... antagonists have been mostly reported to behave in a more or less competitive fashion. Thus, reinforcing the view of ... Angiotensin II Receptors and Angiotensin II Receptor Antagonists, Pharmacological Reviews 45 (1993) 205-247.PubMedGoogle ... Structure-Activity Relationship of the Agonist-Antagonist Transition on the Type 1 Angiotensin II Receptor; the Search for ... 1996) Structure-Activity Relationship of the Agonist-Antagonist Transition on the Type 1 Angiotensin II Receptor; the Search ...
Losartan, an angiotensin type I receptor antagonist, improves conduit vessel endothelial function in Type II diabetes Craig ... Craig CHEETHAM, Gerard ODRISCOLL, Kim STANTON, Roger TAYLOR, Daniel GREEN; Losartan, an angiotensin type I receptor antagonist ... angiotensin receptor blockade, diabetes mellitus, endothelium, flow-mediated dilation, nitric oxide, nitroglycerine ... A type 1 receptor antagonist seems a reasonable alternative to an ACE inhibitor to maintain conduit vessel endothelial function ...
Novel angiotensin II antagonists distinguish amphibian from mammalian angiotensin II receptors expressed in Xenopus laevis ... Novel angiotensin II antagonists distinguish amphibian from mammalian angiotensin II receptors expressed in Xenopus laevis ... Novel angiotensin II antagonists distinguish amphibian from mammalian angiotensin II receptors expressed in Xenopus laevis ... Novel angiotensin II antagonists distinguish amphibian from mammalian angiotensin II receptors expressed in Xenopus laevis ...
Angiotensin II receptor antagonists in the treatment of heart failure: background to and design of the CHARM study. May 2002Br ... in contrast the angiotensin II receptor antagonists (AIIRAs) have failed to demonstrate more than equivalence in randomised ... While angiotensin-converting enzyme (ACE) inhibitors are established agents for the treatment of hypertension and heart failure ...
  • To treat hypertension, a class of Antihypertensive medications called "angiotensin II receptor antagonists" may be prescribed. (blausen.com)
  • It is also used to treat heart failure in people who cannot take angiotensin-converting enzyme (ACE) inhibitors and to reduce the risk of death after a heart attack. (eebb.ru)
  • In order to cause vessel narrowing, angiotensin II binds to proteins, called AT1 receptors, on the surface of smooth muscles within the blood vessels. (blausen.com)
  • By attaching to AT1 receptors on smooth muscle cells lining the blood vessels, this drug blocks angiotensin II from binding. (blausen.com)
  • Losartan was the first, but by no means remained the only, AT1 receptor antagonist. (nih.gov)
  • Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: candesartan 1, telmisartan 10, E3174 (the active metabolite of losartan) 10, tasosartan 20, losartan 50, eprosartan 100 and the prodrug candesartan cilexetil 280. (nih.gov)
  • The angiotensin-II receptor antagonists that have been labeled for use in hypertension by the U.S. Food and Drug Administration (FDA) are losartan (Cozaar), valsartan (Diovan), irbesartan (Avapro), candesartan (Atacand) and telmisartan (Micardis). (aafp.org)
  • To clarify the role of AT 1 and AT 2 receptors, we treated Wistar rats that were infused with Ang II (120 ng/kg/min subcutaneously by osmotic minipump), with the AT 1 antagonist losartan (10 mg/kg/d in the drinking water) and the AT 2 antagonist PD123319 (30 mg/kg/d subcutaneously by osmotic minipump) for 21 days. (ahajournals.org)
  • Two main subtypes of angiotensin receptors have been pharmacologically defined and cloned: AT 1 receptors, which are blocked specifically by losartan, and AT 2 receptors, which are blocked specifically by PD123319. (ahajournals.org)
  • In two successive publications, 7,8 ⇓ investigators obtained results suggesting that when Ang II was infused subcutaneously for 3 weeks into Wistar rats, the increase in blood pressure that occurs in this experimental paradigm is mediated by AT 1 receptors, as shown by abrogation of this effect by concurrent administration of losartan, an AT 1 angiotensin antagonist. (ahajournals.org)
  • We treated Wistar rats that were infused with Ang II (120 ng/kg/min subcutaneously by osmotic minipump), with the AT 1 antagonist losartan (10 mg/kg/d in the drinking water) and/or the AT 2 antagonist PD123319 (30 mg/kg/d subcutaneously by osmotic minipump) for 21 days. (ahajournals.org)
  • Losartan is an ARB that blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II. (medscape.com)
  • Losartan is an orally active, non-peptide Angiotensin II (AT1specific) antagonist. (ijpsonline.com)
  • Results of the studies on losartan and other angiotensin receptor antagonists indicate that they would certainly acquire a commanding position in the treatment of hypertension, a disease that makes millions of people suffer. (ijpsonline.com)
  • Angiotensin converting enzyme genotype influences the response to the angiotensin II receptor antagonist losartan in patients with hypertension. (biomedsearch.com)
  • The angiotensin II (AII) antagonist, losartan, increases uric acid excretion when administered to humans. (aspetjournals.org)
  • However, the active metabolite of losartan, EXP 3174, and other nonpeptide AII antagonists such as eprosartan and SB 203220 are devoid of uricosuric activity. (aspetjournals.org)
  • The other AII antagonists also inhibited urate uptake but were 6-8-fold less potent than losartan with IC50 values of EXP 3174 (65 +/- 13 microM), eprosartan (60 +/- 7.0 microM) and SB 203220 (74 +/- 12.5 microM). (aspetjournals.org)
  • These results suggest that the uricosuric activity of losartan is, at least in part, due to inhibition of urate reabsorption in the proximal tubule and is unrelated to AII receptor activity. (aspetjournals.org)
  • Furthermore, losartan has a greater affinity for the urate/anion exchanger than the other AII antagonists tested. (aspetjournals.org)
  • We have demonstrated previously that inhibition of angiotensin-converting enzyme (ACE) with enalapril and angiotensin II blockade with losartan improve acetylcholine-dependent endothelial function in resistance vessels of patients with Type II diabetes. (portlandpress.com)
  • The angiotensin II receptor antagonist losartan reduces blood pressure but not renal injury in obese Zucker rats. (asnjournals.org)
  • In this study, therefore, the effects of the angiotensin II receptor antagonist losartan on glomerular and tubulointerstitial injury were investigated in obese Zucker rats (OZR), an experimental model of progressive renal disease characterized by reduced intrarenal renin content and reduced plasma renin activity. (asnjournals.org)
  • The effects of ANG II on IPs and [Ca2+]i were inhibited by the ANG II receptor subtype 1 (AT1) antagonist losartan and not by the ANG II receptor subtype 2 (AT2) antagonists PD 123177 and PD 123319. (mysciencework.com)
  • Nephropathy in Type 2 Diabetic Patients: The Reduction of Endpoints in NIDDM with the Angiotensin II Receptor Antagonist Losartan (RENAAL) study was a randomized, placebo-controlled, double-blind, multicenter study conducted worldwide in 1513 patients with type 2 diabetes with nephropathy (defined as serum creatinine 1. (freethesaurus.com)
  • Nonpeptide antagonists of the ATj angiotensin II receptor approved for the treatment of hypertension include losartan (cozaar), candesartan (atacand), irbesartan (avapro), valsartan (diovan), telmisartan (micardis), and eprosartan (teveten). (pharmacologicalsciences.us)
  • The specific AT1 affinity relates to how specificially attracted the medicine is for the correct receptor, the US FDA Package Insert rates for AT1 affinity are as follows: *Losartan 1000 fold *Telmisartan 3000 fold *Irbesartan 8500 fold *Olmesartan 12500 fold *Valsartan 20000 fold 3) The third area that completes the overall efficacy picture of an ARB is half life. (wikidoc.org)
  • title=Comparative efficacy of two angiotensin II receptor antagonists, irbesartan and losartan in mild-to-moderate hypertension. (wikidoc.org)
  • in vitro: Neither the AT1 antagonist losartan nor the AT2 antagonist PD 123319 exhibited significant competition for [125I]angiotensin-(1-7) binding to endothelial cells isolated from bovine aorta, in agreement with the absence of detectable mRNAs encoding typical angiotensin receptor subtypes 1 or 2 (AT1 or AT2) [1]. (apexbt.com)
  • [1] It consists of losartan (an angiotensin II receptor antagonist ) and hydrochlorothiazide (a diuretic ). (wikipedia.org)
  • [3] Losartan works by blocking the effects of angiotensin II while hydrochlorothiazide works by decreasing the ability of the kidneys to absorb electrolytes. (wikipedia.org)
  • However, with coadministration of losartan which is an angiotensin II receptor antagonist, the low levels of potassium are reversed. (wikipedia.org)
  • Background We previously reported that an AT1R antagonist, candesartan, prevents acute electrical remodeling in a rapid pacing model. (onlinejacc.org)
  • The purpose of this study is to determine whether a treatment for diabetic nephropathy, the angiotensin receptor blocker candesartan, modifies mediators of kidney injury independent of blood pressure and the relationships to drug dose. (clinicaltrials.gov)
  • We examined vascular and neural activity in streptozotocin-induced diabetic rats that were treated for 12 weeks with enalapril, an ACE inhibitor, or l -158809, an angiotensin II receptor blocker. (diabetesjournals.org)
  • Kajiya T, Ho C, Wang J, Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. (medchemexpress.com)
  • Azilsartan medoxomil (AZL-M) is a potent angiotensin II receptor blocker that decreases blood pressure in a dose-dependent manner. (elsevier.com)
  • In this study effect of L745,870, a selective D(4) dopamine (DA) receptor blocker, on the pro-cognitive action of intracerebroventricularly (icv) injected angiotensin IV (Ang IV) and des-Phe(6)-Ang IV was examined. (semanticscholar.org)
  • title=Prophylactic treatment of migraine with an angiotensin II receptor blocker: a randomized controlled trial. (wikidoc.org)
  • [8] In a study comparing beta-blocker carvedilol with valsartan, the angiotensin II receptor blocker not only had no deleterious effect on sexual function, but actually improved it. (gutenberg.org)
  • This combination medication contains calcium channel blocker and angiotensin II receptor blocker, prescribed for high blood pressure. (medindia.net)
  • This combination medication contains angiotensin II receptor blocker and diuretic, prescribed for high blood pressure. (medindia.net)
  • Phase A included 1204 patients and was aimed at assessing the efficacy of the angiotensin-converting enzyme (ACE) inhibitor trandolapril, the non-dihydropyridine calcium channel blocker verapamil, and the trandolapril plus verapamil combination as compared with placebo in prevention of microalbuminuria in hypertensive patients with type 2 diabetes and normal urinary albumin excretion rate. (asnjournals.org)
  • We analysed a 10% random sample of all Australian long-term health concession card holders who had been commenced on an angiotensin II receptor antagonist (A2RA), an angiotensin-converting enzyme inhibitor (ACEI) and/or a calcium channel blocker (CCB), but for whom no AHT medication had been dispensed in the previous 6 months. (mja.com.au)
  • At this time, the place for the newest class of antihypertensive drugs, the angiotensin II receptor antagonists, remains uncertain. (aafp.org)
  • Angiotensin II receptor antagonists generally are very well tolerated antihypertensive drugs, but they should be considered as a potential cause of acute reactions, even in patients who have taken them for years. (freethesaurus.com)
  • Finally it provides an overview of the tolerability and compliance profile of the angiotensin II receptor antagonists, a new class of antihypertensive drugs characterized by an efficacy and safety profile. (elsevier.com)
  • Antagonists of angiotensin II receptors, or blockers of AT1 receptors is one of the new groups of antihypertensive drugs. (otc-online-store.com)
  • It is very likely that slow dissociation kinetics from the AT1 receptor underlie insurmountable antagonism. (nih.gov)
  • However, competitive or noncompetitive antagonism does not determine the antihypertensive efficacy, but the slow off-rate may extend the occupancy of the AT1 receptor and thereby lengthen the duration of the antihypertensive effect. (nih.gov)
  • To clarify the role of AT 1 and AT 2 receptors in Ang II-induced growth, we have reproduced in part the experiments reported previously 7 and have examined morphometrically small resistance size arteries in the coronary, renal, mesenteric, and femoral circulation for evidence of growth in presence of AT 1 and AT 2 receptor antagonism. (ahajournals.org)
  • Valsartan is a prodrug that produces direct antagonism of angiotensin II receptors. (medscape.com)
  • It was concluded that in a setting of chronic renal failure where intrarenal RAS activity does not appear to be increased, angiotensin II receptor antagonism may not be nephroprotective despite a reduction in blood pressure. (asnjournals.org)
  • Because the ATj receptor mediates feedback inhibition of renin release, renin and AnglI concentrations are increased during ATJ receptor antagonism. (pharmacologicalsciences.us)
  • IC50 Value: 0.62 nM [2] Target: AT1 receptor in vitro: In aortic endothelial cells, azilsartan inhibited cell proliferation at concentrations as low as 1 μmol/l, whereas valsartan showed little or no antiproliferative effects at concentrations below 10 μmol/l. (medchemexpress.com)
  • Valsartan is a type of medicine called an angiotensin II receptor antagonist. (netdoctor.co.uk)
  • Valsartan works by preventing the action of a hormone in the body called angiotensin II. (netdoctor.co.uk)
  • Valsartan blocks the receptors that angiotensin II acts on and so prevents its actions. (netdoctor.co.uk)
  • Tolvaptan (Jynarque), a selective vasopressin V2-receptor antagonist, was approved by the US.Food and Drug Administration (FDA) in April 2018 to slow kidney function decline in adults at risk of rapidly progressing autosomal dominant polycystic kidney disease (ADPKD). (medscape.com)
  • The selective vasopressin V2-receptor antagonist, tolvaptan, causes an increase in urine water excretion that results in an increase in free water clearance (aquaresis), a decrease in urine osmolality, and a resulting increase in serum sodium concentration. (medscape.com)
  • EMA401, an orally administered highly selective angiotensin II type 2 receptor antagonist, as a novel treatment for postherpetic neuralgia: a randomised, double-blind, placebo-controlled phase 2 clinical trial. (painresearchforum.org)
  • EMA401, a highly selective AT2R antagonist, is under development as a novel neuropathic pain therapeutic agent. (semanticscholar.org)
  • One notable exception is the angiotensin II type 2 (AT2) receptor that has clinical validity on the basis of a successful double-blind, randomized, placebo-controlled, clinical trial of EMA401, a highly selective, orally active, peripherally restricted AT2 receptor antagonist in patients with postherpetic neuralgia. (ovid.com)
  • PD 123319 (ditrifluoroacetate) is a potent, selective AT2 angiotensin II receptor antagonist with IC 50 of 34 nM. (medchemexpress.com)
  • Description: IC50 Value: 1.2 ±0.4 mM (Inhibition of adenylyl cyclase elicited by 0.1 microM Ang II) [2] PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. (apexbt.com)
  • Suzuki H, Kanno Y, Sugahara S, Ikeda N, Shoda J, Takenaka T, Inoue T, Araki R. Effect of angiotensin receptor blockers on cardiovascular events in patients undergoing hemodialysis: an open-label randomized controlled trial. (clinicaltrials.gov)
  • Objectives The purpose of the present study was to evaluate the effect of angiotensin II type 1 receptor (AT1R) antagonist on chronic structural remodeling in atrial fibrillation (AF). (onlinejacc.org)
  • No effect of angiotensin II AT(2)-receptor antagonist PD 123319 on cerebral blood flow autoregulation. (medchemexpress.com)
  • This medication is an ACE (angiotensin-converting enzyme) inhibitor, prescribed for high blood pressure either alone or with other medications. (medindia.net)
  • To assess the chronic antihypertensive and renal protective effects of the specific angiotensin II receptor antagonist, CS-866, in the remnant kidney model of chronic renal failure, we administered it alone or in combination with temocapril, an angiotensin converting enzyme inhibitor, to 5/6 nephrectomized spontaneously hypertensive rats (SHR) for 8 weeks. (elsevier.com)
  • 2: Tokioka-Akagi T, Fujimori A, Shibasaki M, Inagaki O, Yanagisawa I. Comparison of the angiotensin II type 1-receptor antagonist YM358 and the angiotensin-converting enzyme inhibitor enalapril in rats with cardiac volume overload. (medkoo.com)
  • Why Book A Pittsburgh generic angiotensin ii receptor antagonists replacements through GigMasters? (xlx.pl)
  • gait assessment: moredifficult because of generic angiotensin ii receptor blockers concurrentmusculoskeletal unwellness andpre-existing neurologicaldeficits. (billupselite.com)
  • Hydrochlorothiazide - are there any angiotensin drugs that dont include hydrochothiazide? (drugs.com)
  • origination of ldl aphaeresis should generallybe retarded angiotensin receptor blockers nz until more or less 5 years of age, leave off whenevidence of coronary-artery disease avascular illness is present. (dustbowltough.com)
  • 2 Angiotensin-II receptor antagonists act by binding to specific membrane-bound receptors that displace A-II from its type 1-receptor subtype (AT 1 ). (aafp.org)
  • Angiotensin II (Ang II) appears to exert its contractile and growth-promoting effects through the AT 1 receptor subtype, whereas the AT 2 subtype may have growth-inhibitory and proapoptotic properties. (ahajournals.org)
  • No evidence for AT2 receptor subtype is found. (mysciencework.com)
  • The ATj receptor subtype is located predominantly in vascular and myocardial tissue and also in brain, kidney, and adrenal glomerulosa cells, which secrete aldosterone (see Chapter 30). (pharmacologicalsciences.us)
  • These results demonstrate that AT1 receptor subtypes are present in intact rat proximal tubule cells and are coupled to both IPs-Ca2+ and cAMP signaling pathways. (mysciencework.com)
  • Distinct subtypes of AnglI receptors are designated as ATj and AT2. (pharmacologicalsciences.us)
  • Other poorly characterized subtypes include the AT 3 and AT 4 receptors. (wikipedia.org)
  • Disposition of the angiotensin II receptor antagonist L-158,809 in rats and rhesus monkeys. (aspetjournals.org)
  • Dopamine D4 receptor antagonist L745,870 abolishes cognitive effects of intracerebroventricular angiotensin IV and des-Phe(6)-Ang IV in rats. (semanticscholar.org)
  • Hippocampal asymmetry in angiotensin II modulatory effects on learning and memory in rats. (semanticscholar.org)
  • In animal studies, Cameron and colleagues ( 7 - 10 ) have demonstrated that treating streptozotocin-induced diabetic rats with lisinopril or an angiotensin II receptor antagonist improved nerve function and modulated nerve blood flow. (highwire.org)
  • 1: Oka-Akagi T, Fujimori A, Shibasaki M, Matsuda-Satoh Y, Inagaki O, Yanagisawa I. Effects of angiotensin II type 1 receptor antagonist, YM358, on cardiac hypertrophy and dysfunction after myocardial infarction in rats. (medkoo.com)
  • 8: Yamaguchi N, Fujimoto K, Fujii T, Suzuki T, Kawashima K. Antihypertensive effect of repeatedly administered YM358, an angiotensin AT1-receptor antagonist, in stroke-prone spontaneously hypertensive rats. (medkoo.com)
  • AT 2 receptors are found in many tissues, including those of the adrenal medulla, uterus, ovary and other brain regions, but they are not known to be related to cardiovascular homeostasis. (aafp.org)
  • Ang II, the final mediator of the renin-angiotensin system, plays a pivotal physiological role in cardiovascular homeostasis. (ahajournals.org)
  • ACE inhibition and/or blocking of the angiotensin II receptor are recognized as first-line treatment for nephropathy and cardiovascular disease in diabetic patients. (diabetesjournals.org)
  • Angiotensin AT2 receptors: cardiovascular hope or hype? (exposurebiz.com)
  • This agent prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower aldosterone secretion. (medscape.com)
  • [11] The system increases blood pressure by increasing the amount of salt and water the body retains, although angiotensin is also very good at causing the blood vessels to tighten (a potent vasoconstrictor ). (wikipedia.org)
  • A few years later, the concept of a system specifically involved in BP control came to the light with discovery by Page and Braun-Menendez that renin is a peptidase that produces the vasoconstrictor peptide angiotensin II from the precursor angiotensinogen ( 3 ). (asnjournals.org)
  • We previously reported that the blockade of angiotensin II (Ang II) prevented the electrical remodeling induced by short-term rapid atrial pacing (4) . (onlinejacc.org)
  • Recent attention has focused on understanding the role of the brain-renin-angiotensin-system (RAS) in stroke and neurodegenerative diseases. (biomedcentral.com)
  • Efficacy of angiotensin II receptor antagonists in preventing headache: a systematic overview and meta-analysis. (acpjc.org)
  • In this study, we review research to date on target validation, efficacy, and mode of action of small molecule AT2 receptor antagonists in rodent models of peripheral neuropathic pain and in cultured human sensory neurons, the preclinical pharmacokinetics of these compounds, and the outcome of the above clinical trial. (ovid.com)
  • Recent trials have now shown that treatment with beta-blockers, aldosterone antagonists and angiotensin receptor blockers also leads to substantial improvements in outcome. (nih.gov)
  • M. C. Sharma and D. V. Kohli, "3D QSAR studies on a series of sulfonylcarbamate isostere derivatives as non-peptide angiotensin II receptor antagonists: kNNMFA method," American-Eurasian Journal of Agricultural & Environmental Sciences , vol. 6, no. 2, pp. 64-70, 2011. (hindawi.com)
  • In contrast to the effects of the nonpeptide AII antagonists, the peptide antagonist, Sar1,Ile8-AII, as well as AII itself had no effect on urate uptake. (aspetjournals.org)
  • Angiotensin II is the main effector peptide of the RAAS. (otc-online-store.com)
  • The angiotensin receptor is activated by the vasoconstricting peptide angiotensin II . (wikipedia.org)
  • In contrast, medial hypertrophy of aorta and coronary arteries was abolished by concomitant administration of the AT 2 receptor antagonist PD123319. (ahajournals.org)
  • Effects mediated by the AT 2 receptor are suggested to include inhibition of cell growth , fetal tissue development, modulation of extracellular matrix, neuronal regeneration, apoptosis , cellular differentiation , and maybe vasodilation and left ventricular hypertrophy . (wikipedia.org)
  • Angiotensin II may also induce mesangial and vascular cell hypertrophy ( 14 ) and sustain chronic inflammation, ischemia, and fibrosis in proteinuric kidneys ( 15 ). (asnjournals.org)
  • Activation of the AT 1 -receptor is involved in vasoconstriction, inactivation of bradykinin, water and salt homeostasis, reactive oxygen species production, cellular hypertrophy and hyperplasia, and apoptosis ( 14 ). (highwire.org)
  • (1) observed that the activation of angiotensin-converting enzyme (ACE)-dependent extracellular signal-regulated kinases (Erk1/Erk2) was involved in the mechanism of the development of atrial fibrosis in patients with AF. (onlinejacc.org)
  • 3 AT-II pressor effects are mediated by AT 1 receptors. (aafp.org)
  • the results show little evidence of a role of AT 2 receptors in mediating angiotensin II effects in this experimental paradigm. (ahajournals.org)
  • Meta-analysis using a random-effects model showed that patients who received angiotensin II receptor antagonists had a lower risk for headache than did patients who received placebo (Table). (acpjc.org)
  • Effects of angiotensin II and nonpeptide receptor antagonists. (mysciencework.com)
  • Effects of angiotensin II and nonpeptide receptor antagonists on transduction pathways in rat proximal tubule. (mysciencework.com)
  • Antiproliferative effects of azilsartan were also observed in cells lacking AT1 receptors[1]. (medchemexpress.com)
  • The angiotensin II receptor blockers have differing potencies in relation to blood pressure control, with statistically differing blood pressure effects at the maximal doses. (wikidoc.org)
  • This study evaluates prospectively the effects of an anti-angiotensin II regimen on renal outcome in patients with mesangioproliferative glomerulonephritis followed-up for 10 years. (clinicaltrials.gov)
  • Most known effects of angiotensin II are mediated via activation of the AT 1 -receptor. (highwire.org)
  • Which medications in the drug class Angiotensin II receptor antagonists are used in the treatment of IgA Nephropathy? (medscape.com)
  • The present invention relates to use of an ACE inhibitor and/or angiotensin II receptor antagonist of the preparation of a medicament for the treatment of skin ageing or wrinkling. (allindianpatents.com)
  • Design and rationale of a prospective, collaborative meta-analysis of all randomized controlled trials of angiotensin receptor antagonists in Marfan syndrome, based on individual patient data: A report from the Marfan Treatment Trialists' Collaboration. (cdc.gov)
  • We believe to possess the necessary tools (enlarged but planar aromatic side-chains in position 8) in order to explore the concept of inverse agonism on the mammalian AT1 receptor. (springer.com)
  • Whether RAS antagonists affect renal disease progression when intrarenal RAS activity is not increased is unclear. (asnjournals.org)