Angiotensin receptor antagonists. Medical search

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)

... angiotensin II receptor antagonists may be useful because they act to prevent the action of angiotensin II at the AT1 receptor ... "Pregnancy Outcome Following Exposure to Angiotensin-Converting Enzyme Inhibitors or Angiotensin Receptor Antagonists: A ... Angiotensin II receptor antagonistsEdit. ACE inhibitors possess many common characteristics with another class of ... The combination therapy of angiotensin II receptor antagonists with ACE inhibitors may be superior to either agent alone. This ...

https://en.m.wikipedia.org/wiki/ACE_inhibitors

... is an angiotensin II receptor antagonist. It was withdrawn from FDA review by the manufacturer after phase III ... ISBN 978-0-12-369417-1. Dina R, Jafari M (July 2000). "Angiotensin II-receptor antagonists: an overview". Am J Health Syst ...

https://en.wikipedia.org/wiki/Tasosartan

However, with coadministration of losartan which is an angiotensin II receptor antagonist, the low levels of potassium are ... Losartan works by blocking the effects of angiotensin II by preventing it from binding to the angiotensin I receptor while ... an angiotensin II receptor antagonist) and hydrochlorothiazide (a diuretic).[1] It is taken by mouth.[1] ... Losartan works by blocking the effects of angiotensin II while hydrochlorothiazide works by decreasing the ability of the ...

https://en.wikipedia.org/wiki/Hyzaar

Olmesartan is an angiotensin II receptor antagonist and blocks part of the RAAS pathway. Amlodipine/perindopril if using ... Amlodipine-association edema can be avoided by adding ACE inhibitors or angiotensin II receptor antagonist. Of the other dose- ... Amlodipine/valsartan or amlodipine/valsartan/hydrochlorothiazide, where valsartan is an angiotensin II receptor antagonist. The ... Amlodipine/telmisartan, where telmisartan is an angiotensin II receptor antagonist. ...

https://en.wikipedia.org/wiki/Amlodipine

... , 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 ...

https://en.wikipedia.org/wiki/Forasartan

"Nonpeptide angiotensin II receptor antagonists: the next generation in antihypertensive therapy". Journal of Medicinal ... More recently angiotensin receptor blockers and renin inhibitors have also been introduced as antihypertensive agents. Esunge ... The renin-angiotensin system was known to play an important role in blood pressure regulation, and angiotensin converting ... Ondetti MA, Rubin B, Cushman DW (April 1977). "Design of specific inhibitors of angiotensin-converting enzyme: new class of ...

https://en.wikipedia.org/wiki/History_of_hypertension

It is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II. It was patented in 1991 and ... In studies of angiotensin II receptor antagonists such as olmesartan, patients with unilateral or bilateral renal artery ... Aulakh, GK; Sodhi, RK; Singh, M (2 August 2007). "An update on non-peptide angiotensin receptor antagonists and related RAAS ... "Angiotensin II receptor blocker induced fetopathy: 7 cases". Klin Padiatr. 223 (1): 10-4. doi:10.1055/s-0030-1269895. PMID ...

https://en.wikipedia.org/wiki/Olmesartan

Coca A (2008). "Economic benefits of treating high-risk hypertension with angiotensin II receptor antagonists (blockers)". ... Raebel MA (June 2012). "Hyperkalemia associated with use of angiotensin-converting enzyme inhibitors and angiotensin receptor ... Subsequently, beta blockers, calcium channel blockers, angiotensin converting enzyme (ACE) inhibitors, angiotensin receptor ... and angiotensin receptor blockers (ARBs). These medications may be used alone or in combination (ACE inhibitors and ARBs are ...

https://en.wikipedia.org/wiki/Hypertension

AbdAlla S, Lother H, Abdel-tawab AM, Quitterer U (2001). "The angiotensin II AT2 receptor is an AT1 receptor antagonist". J. ... Shraga-Levine Z, Sokolovsky M (2000). "Functional coupling of G proteins to endothelin receptors is ligand and receptor subtype ... 1996). "The human thyrotropin receptor: a heptahelical receptor capable of stimulating members of all four G protein families ... Offermanns S, Simon MI (1995). "G alpha 15 and G alpha 16 couple a wide variety of receptors to phospholipase C". J. Biol. Chem ...

https://en.wikipedia.org/wiki/GNA11

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 ...

https://en.wikipedia.org/wiki/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 ...

https://en.wikipedia.org/wiki/Bezold–Jarisch_reflex

Other reasonable initial options include angiotensin II receptor antagonists, calcium-channel blockers, and thiazide diuretics ... It is an ACE inhibitor and works by decreasing renin-angiotensin-aldosterone system activity. Benazepril was patented in 1981 ... Dykewicz, Mark S. (April 2004). "Cough and Angioedema From Angiotensin-Converting Enzyme Inhibitors: New Insights Into ... and inhibition of plasma angiotensin-converting enzyme activity after single and repeated administrations to dogs". Am. J. Vet ...

https://en.wikipedia.org/wiki/Benazepril

It is an angiotensin II receptor antagonist and works by blocking the effects of angiotensin II. Valsartan was patented in 1990 ... The drug binds to angiotensin type I receptors (AT1), working as an antagonist. This mechanism of action is different than that ... As valsartan acts at the receptor, it can provide more complete angiotensin II antagonism since angiotensin II is generated by ... There is contradictory evidence with regard to treating people with heart failure with a combination of an angiotensin receptor ...

https://en.wikipedia.org/wiki/Valsartan

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 & ...

https://en.wikipedia.org/wiki/IgA_nephropathy

... is an angiotensin II receptor antagonist used for the treatment of high blood pressure. It is marketed in the United ... As with other angiotensin II receptor antagonists, eprosartan is generally better tolerated than enalapril (an ACE inhibitor), ... First, it blocks the binding of angiotensin II to AT1 receptors in vascular smooth muscle, causing vascular dilatation. Second ... Discovery and development of angiotensin receptor blockers Anon., 2006, Abbott Laboratories: Kos Pharmaceuticals a wise buy, ...

https://en.wikipedia.org/wiki/Eprosartan

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 ...

https://en.wikipedia.org/wiki/Telmisartan

Those who cannot tolerate ACE inhibitors may be treated with an angiotensin II receptor antagonist. Statin therapy has been ... Aldosterone antagonists appear to be useful in people who have had an STEMI and do not have heart failure. Cardiac ... Aldosterone antagonists (spironolactone or eplerenone) may be used if there is evidence of left ventricular dysfunction after ... July 2018). "Aldosterone Antagonist Therapy and Mortality in Patients With ST-Segment Elevation Myocardial Infarction Without ...

https://en.wikipedia.org/wiki/Myocardial_infarction

... is an angiotensin II receptor antagonist used in the treatment of hypertension, developed by Takeda. It is marketed ... Azilsartan medoxomil lowers blood pressure by blocking the action of angiotensin II at the AT1 receptor, a hormone that ... Like other antihypertensive drugs acting on the renin-angiotensin system, it is contraindicated during the second and third ... Based on experiences with other drugs acting on the renin-angiotensin system, it is theorized that azilsartan could increase ...

https://en.wikipedia.org/wiki/Azilsartan

Coca A. Economic benefits of treating high-risk hypertension with angiotensin II receptor antagonists (blockers). Clinical Drug ... 2.5.5.1 Angiotensin-converting enzyme inhibitors. British National Formulary No. 62. September 2011 [2011-12-22].. [永久失效連結] ... Role of the renin-angiotensin system in vascular inflammation. Trends Pharmacol. Sci. July 2008, 29 (7): 367-74. PMID 18579222 ... Counterpoint: Activation of the intrarenal renin-angiotensin system is the dominant contributor to systemic hypertension. J. ...

https://zh.wikipedia.org/zh-tw/高血壓

Coca A (2008). "Economic benefits of treating high-risk hypertension with angiotensin II receptor antagonists (blockers)". ... Pedoman ini menyarankan penghambat enzim konversi angiotensin (angiotensin-converting enzyme inhibitor/ACEI) yang merupakan ... Dua jenis penghambat sistem renin-angiotensin (contohnya, penghambat enzim konversi angiotensin + penghambat reseptor ... "2.5.5.1 Angiotensin-converting enzyme inhibitors". British National Formulary. No. 62. September 2011. Diakses tanggal 2011-12- ...

https://id.wikipedia.org/wiki/Hipertensi

Coca A (2008). "Economic benefits of treating high-risk hypertension with angiotensin II receptor antagonists (blockers)". ... "2.5.5.1 Angiotensin-converting enzyme inhibitors". British National Formulary. No. 62. September 2011. Erişim tarihi: 22 Aralık ... Zeng C, Villar VA, Yu P, Zhou L, Jose PA (April 2009). "Reactive oxygen species and dopamine receptor function in essential ... Marchesi C, Paradis P, Schiffrin EL (July 2008). "Role of the renin-angiotensin system in vascular inflammation". Trends ...

https://tr.wikipedia.org/wiki/Yüksek_tansiyon

... is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. ... fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as ... Angiotensin-converting enzyme (ACE) then catalyzes the reaction that forms angiotensin II, which acts on AT1 receptors on the ... Harada K, Sugaya T, Murakami K, Yazaki Y, Komuro I (November 1999). "Angiotensin II type 1A receptor knockout mice display less ...

https://en.wikipedia.org/wiki/Fimasartan

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 ...

https://en.wikipedia.org/wiki/Outline_of_cardiology

... angiotensin II receptor antagonists or adrenergic antagonists. Elevated lipid levels, including HDL, were found to increase ... receptor antagonist; cholinesterase inhibitors galantamine, donepezil, rivastigmine; Studies have shown that an extract of ... These medications include angiotensin converting enzyme inhibitors, diuretics, calcium channel blockers, sympathetic nerve ...

https://en.wikipedia.org/wiki/Vascular_dementia

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 ...

https://en.wikipedia.org/wiki/Saralasin

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. ...

https://en.wikipedia.org/wiki/MAS1_oncogene

... simple procedures for the large-scale preparation of buildings blocks for angiotensin (II) receptor antagonists", Liebigs Ann. ... which bind to peroxisome-proliferator-activated receptors (PPARγ) and activate the expression of a variety of genes): In a ... in the build up of pharmacologically active biphenyl compounds such as a precursor of the antihypertensive AT1 antagonist ...

https://en.wikipedia.org/wiki/4-Formylphenylboronic_acid

It is a reagent used in the synthesis of tetrazoles, which in turn are used to generate angiotensin II receptor antagonists. In ...

https://en.wikipedia.org/wiki/Tributyltin_azide

... an angiotensin II receptor antagonist. Within three weeks, she began experiencing a metallic taste and a burning sensation in ... Each taste bud contains receptor cells. Afferent nerves make contact with the receptor cells at the base of the taste bud. A ... Drugs that act by blocking the renin - angiotensin - aldosterone system, for example by antagonizing the angiotensin II ... including transport of tastes to the receptor and protection of the taste receptor. Typical clinical investigations involve ...

https://en.wikipedia.org/wiki/Dysgeusia

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 ...

https://en.wikipedia.org/wiki/GABAA_receptor_positive_allosteric_modulator

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 ...

https://en.m.wikipedia.org/wiki/Receptor_

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 ...

https://en.wikipedia.org/wiki/FZD5

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. ...

https://en.m.wikipedia.org/wiki/Diuretic

... 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. ...

https://en.wikipedia.org/wiki/Fenoldopam

ACE inhibitors, angiotensin receptor blockers, direct renin inhibitors and aldosterone antagonists, are pharmacological ...

https://en.wikipedia.org/wiki/Hypertensive_nephropathy

... 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) ...

https://en.wikipedia.org/wiki/Bradykinin

D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... Prolactin modulators: Prolactin inhibitors: D2 receptor agonists (e.g., bromocriptine, cabergoline); Prolactin releasers: ...

https://en.wikipedia.org/wiki/Puromycin

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 ...

https://en.m.wikipedia.org/wiki/Pharmaceutical

... 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 ...

https://en.wikipedia.org/wiki/Insulin-like_growth_factor_2

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 ...

https://en.wikipedia.org/wiki/Antiemetic

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: ...

https://en.wikipedia.org/wiki/Icatibant

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 ...

https://id.wikipedia.org/wiki/Asthma

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 ...

https://en.m.wikipedia.org/wiki/Drug_class

The conversion of angiotensin I to angiotensin II and the inactivation of bradykinin were thought to be mediated by the same ... Receptor. (ligands). BLT. BLT1. *Agonists: 12-HETE. *20-Hydroxy-LTB4 ... Antagonists: 20-Carboxy-LTB4. *Amelubant. *CGS-23131 (LY-223982). *CGS-25019C ... Ng KK, Vane JR (November 1967). "Conversion of angiotensin I to angiotensin II". Nature. 216 (5117): 762-6. Bibcode:1967Natur. ...

https://en.wikipedia.org/wiki/Captopril

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 ...

https://en.wikipedia.org/wiki/Adrenocorticotropic_hormone

https://en.wikipedia.org/wiki/Glucagon-like_peptide_2

... 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 ...

https://en.wikipedia.org/wiki/Primary_polydipsia

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 ...

https://en.wikipedia.org/wiki/Adenosine_receptor

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 ...

https://en.wikipedia.org/wiki/CCK-4

Angiotensin receptor antagonists[2]. losartan, valsartan -pril. Angiotensin converting enzyme inhibitor[2]. captopril, ... Leukotriene receptor antagonists[2]. zafirlukast, montelukast -grel-. Platelet aggregation inhibitor[2]. clopidogrel, ...

https://tl.wikipedia.org/wiki/Nomenklatura_ng_gamot

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 ...

https://en.wikipedia.org/wiki/Algesic

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 ...

https://en.wikipedia.org/wiki/Stimulants

Competitive NMDA receptor antagonists[edit]. Competitive NMDA receptor antagonists, which were developed first, are not a good ... 7.5 Development of NMDA receptor antagonists *7.5.1 Competitive NMDA receptor antagonists ... Development of NMDA receptor antagonists[edit]. The main problem with the development of NMDA antagonists for neuroprotection ... The N-methyl-D-aspartate receptor (also known as the NMDA receptor or NMDAR), is a glutamate receptor and ion channel found in ...

https://en.wikipedia.org/wiki/NMDA_receptor

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. ...

https://en.wikipedia.org/wiki/Chemotherapeutics

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 ...

https://en.wikipedia.org/wiki/Decongestant

... (INN) (code name MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational ... "Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine". Neurology. 70 (16): ... D2 receptor antagonists (e.g., domperidone, metoclopramide, risperidone) ... a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised ...

https://en.wikipedia.org/wiki/Telcagepant

"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 ...

https://ml.wikipedia.org/wiki/പ്രോസ്റ്റാഗ്ലാൻഡിൻ_EP3_റിസപ്റ്റർ

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 ...

https://en.wikipedia.org/wiki/Galanin_receptor_1

Pharmacological properties of angiotensin II receptor antagonists.. Timmermans PB1.. Author information. 1. Tularik Inc, South ... receptor antagonists has provided the opportunity to obtain the benefits of selectively blocking the renin-angiotensin- ... Losartan was the first, but by no means remained the only, AT1 receptor antagonist. Numerous other sartans have emerged in ... Among the current AT1 receptor antagonists, the rank order of the relative binding affinities (highest affinity = 1) is: ...

https://www.ncbi.nlm.nih.gov/pubmed/10579749?dopt=Abstract

Angiotensin-II receptor antagonists are well tolerated. Cough occurs much less often with these agents than with angiotensin- ... Clinical trials indicate that angiotensin-II receptor antagonists are effective and safe in the treatment of hypertension. ... These drugs are selective for angiotensin II (type 1 receptor); unlike angiotensin-converting enzyme inhibitors, they do not ... Angiotensin-II receptor antagonists (or blockers) are a newer class of antihypertensive agents. ...

http://www.aafp.org/afp/1999/0601/p3140.html

Angiotensin Receptor Antagonists to Prevent Sudden Death in Heart Failure: Does the Dose Matter?. Pietro Francia,1 Francesca ... Pietro Francia, Francesca Palano, Giuliano Tocci, et al., "Angiotensin Receptor Antagonists to Prevent Sudden Death in Heart ...

https://www.hindawi.com/journals/isrn/2014/652421/cta/

When data from ongoing trials become available, angiotensin II receptor antagonists may prove to be a good choice for initial ... At this time, the place for the newest class of antihypertensive drugs, the angiotensin II receptor antagonists, remains ... Currently, they are considered reasonable alternatives for patients who have a compelling need for an angiotensin-converting ... Angiotensin II antagonists block all of the known actions of angiotensin II, acting on the cell receptors identified as the AT1 ...

https://www.aafp.org/afp/1999/0915/p1185.html

The aim of the present microiontophoretic study of angiotensin II-sensitive rat paraventricular neu … ... In comparison with angiotensin III this excitatory action was significantly delayed. ... In a previous study we observed that most neurones in the paraventricular nucleus are excited by angiotensin-(1-7). ... angiotensin II and angiotensin III could always be inhibited with both angiotensin receptor subtype antagonists 1 and 2, that ...

https://pubmed.ncbi.nlm.nih.gov/1574605/?dopt=Abstract

... "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 ...

https://blausen.com/en/video/angiotensin-ii-receptor-antagonists/

Nonpeptide angiotensin II receptor antagonist that blocks the... more ... Angiotensin II receptor antagonistsReduce blood pressure and proteinuria, protect renal function, and delay onset of ESRD. ... Nonpeptide angiotensin II receptor antagonist that blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin ... Angiotensin II receptor antagonists. Reduce blood pressure and proteinuria, protect renal function, and delay onset of ESRD. ...

https://www.medscape.com/answers/239927-81575/which-medications-in-the-drug-class-angiotensin-ii-receptor-antagonists-are-used-in-the-treatment-of-iga-nephropathy

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 ...

http://hyper.ahajournals.org/content/31/1/487

... , heart failure, hypertension, Renin-angiotensin system ... Filed Under: People, Places & Events, Policy & Ethics Tagged With: Angiotensin II receptor antagonist, Celiac Disease, diarrhea ... Filed Under: Prevention, Epidemiology & Outcomes Tagged With: ace inhibitor, Angiotensin II receptor antagonist, ... Angiotensin II receptor antagonist, European Medicines Agency, food and drug administration, heart failure, hypertension ...

https://www.cardiobrief.org/tag/angiotensin-ii-receptor-antagonist/

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 ...

https://emedicine.medscape.com/article/244907-medication

... receptor antagonist (ab120997) has been cited in 4 publications. Find out more about the references ... Oliveira PA et al. Angiotensin II type 1/adenosine A 2A receptor oligomers: a novel target for tardive dyskinesia. Sci Rep 7: ... Ageeva LV et al. Data supporting that adipose-derived mesenchymal stem/stromal cells express angiotensin II receptors in situ ... Agonists, activators, antagonists and inhibitors. Lysates. Multiplex Assays. By research area. Cancer. Cardiovascular. Cell ...

https://www.abcam.com/losartan-potassium-non-peptide-angiotensin-ii-at1-receptor-antagonist-ab120997-references.html

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.. ...

https://insights.ovid.com/hypertension/jhype/1994/12/000/angiotensin-receptor-antagonists-treatment/3/00004872

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/ ...

https://www.ncbi.nlm.nih.gov/pubmed/16087129?dopt=Abstract

Effects of Specific Antagonists of Angiotensin II Receptors and Captopril on Diabetic Nephropathy in Mice * * Yotsumoto Takashi ... Comparison of inhibitory potency by nonpeptide angiotensin II receptor antagonists PD123177 and DuP 753 on proximal nephron and ... The 35-day treatments of captopril and Dup 753 (angiotensin II type 1 receptor antagonist) significantly attenuated the ... These results suggest that angiotensin II type 2 receptor as well as type 1 receptor may be involved in the development of ...

https://ci.nii.ac.jp/naid/10008679737

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 ...

https://clinicaltrials.gov/show/NCT00530595

... 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 ...

https://www.ijpsonline.com/abstract/angiotensin-receptor-antagonists-a-new-class-of-antihypertensive-drugs-1886.html

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 ...

https://www.hindawi.com/journals/jchem/2013/427181/ref/

... 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 ...

https://emedicine.medscape.com/article/152696-medication

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 ...

http://diabetes.diabetesjournals.org/content/55/2/341

Angiotensin II receptor antagonists (ARBs, sartans) by level of risk according e-lactancia.org ... Angiotensin II receptor antagonists (ARBs, sartans). *ATC C02(A-K): Anti-hypertensive Anti Alpha-adrenergics, Vasodilators & ...

http://e-lactancia.org/breastfeeding/atc-c09c-anti-hypertensive-angiotensin-ii-receptor-antagonists-arbs-sartans/group/

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 ...

http://hyper.ahajournals.org/content/39/2/375

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 ...

https://annals.org/aim/article-abstract/744503/current-guidelines-using-angiotensin-converting-enzyme-inhibitors-angiotensin-ii-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. ...

http://jpet.aspetjournals.org/content/276/1/125

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 ...

http://www.biomedsearch.com/nih/Angiotensin-converting-enzyme-genotype-influences/15080371.html

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. ...

http://ci.nii.ac.jp/naid/10008191538

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 ...

http://jpet.aspetjournals.org/content/early/2003/08/27/jpet.103.053322

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 ...

http://acpjc.org/Content/138/1/issue/ACPJC-2003-138-1-012.htm

Antagonist activity at rat AT1 receptor expressed in CHO cells assessed as angiotensin 2-evoked increase in intracellular ...

https://pubchem.ncbi.nlm.nih.gov/bioassay/320852

... 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 ...

https://link.springer.com/chapter/10.1007/978-1-4899-1376-0_14

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 ...

https://portlandpress.com/clinsci/article-abstract/100/1/13/66431/Losartan-an-angiotensin-type-I-receptor-antagonist?redirectedFrom=fulltext

The availability of selective, potent, orally active and long acting nonpeptide angiotensin II type 1 (AT1) receptor antagonists has provided the opportunity to obtain the benefits of selectively blocking the renin-angiotensin-aldosterone system at the level of the AT1 receptor that mediates most, if not all, of the important actions of angiotensin II, and avoid the nonspecificity of the angiotensin I converting enzyme inhibitors. (nih.gov)
The renin-angiotensin-aldosterone system plays an integral role in the pathophysiology of hypertension because it affects the regulation of fluid volume, electrolyte balance and blood volume. (aafp.org)
Components of the renin-angiotensin-aldosterone system and sites at which angiotensin-converting enzyme (ACE) inhibitors work and angiotensin-II receptor antagonists interrupt the type 1-receptor subtype (AT 1 ) of angiotensin II. (aafp.org)
ACE inhibitors suppress the renin-angiotensin-aldosterone system. (medscape.com)
It unites drugs that modulate the functioning of the renin-angiotensin-aldosterone system (RAAS) through interaction with angiotensin receptors. (otc-online-store.com)
Renin-angiotensin-aldosterone system is a major blood pressure regulating mechanism. (wikipedia.org)
Angiotensin II receptor antagonists (ARBs) modulate the function of the renin-angiotensin-aldosterone system and are commonly prescribed antihypertensive drugs, especially in patients with renal failure. (ac.rs)
Angiotensin II receptor antagonists , also known as angiotensin receptor blockers (ARBs) , AT 1 -receptor antagonists or sartans , are a group of pharmaceuticals that modulate the renin-angiotensin-aldosterone system . (gutenberg.org)

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)
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)
Angiotensin converting enzyme genotype influences the response to the angiotensin II receptor antagonist losartan in patients with hypertension. (biomedsearch.com)
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)
One drug (losartan, an ARB) has been shown in a recent publication (below) to act as a CCR2 antagonist to block monocyte migration, which when sustained leads to tumor macrophage depletion. (csuventures.org)
The Angiotensin Receptor Blocker Losartan Suppresses Growth of Pulmonary Metastases via AT1R-Independent Inhibition of CCR2 Signaling and Monocyte Recruitment. (csuventures.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)
Segment by Type Valsartan Telmisartan Losartan Irbesartan Azilsartan Olmesartan Segment by Application Hypertension Cardiovascular Diseases Kidney Diseases Other The Angiotensin Receptor Antagonists market is analysed and market size information is provided by regions (countries). (marketstudyreport.com)
An angiotensin 2 receptor antagonist known as losartan (marketed as Cozaar , manufactured by Merck ) is commonly used as an alternative to calcium channel blockers in treating Raynaud's phenomenon. (sclerodermanews.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)

unlike angiotensin-converting enzyme inhibitors, they do not inhibit bradykinin metabolism or enhance prostaglandin synthesis. (aafp.org)
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. (aafp.org)
The effect of A-II is likely to be more completely blocked by the AT 1 receptor antagonism of angiotensin-II receptor blockers than by ACE inhibitors. (aafp.org)
May induce a more complete inhibition of the renin-angiotensin system than ACE inhibitors, do not affect the response to bradykinin, and are less likely to be associated with cough and angioedema. (medscape.com)
The enormous success of ACE inhibitors in hypertension and heart failure spurred hope that adding a second drug to block the renin-angiotensin system would yield improved outcomes. (cardiobrief.org)
The drugs of choice for hypertension related to ADPKD are angiotensin-converting enzyme (ACE) inhibitors and angiotensin II receptor blockers (ARBs). (medscape.com)
Practical recommendations for the use of ACE inhibitors, beta-blockers, aldosterone antagonists and angiotensin receptor blockers in heart failure: putting guidelines into practice. (nih.gov)
Angiotensin receptor blockers are as effective as ACE inhibitors in the treatment of heart failure. (medscape.com)
It may induce more complete inhibition of the renin-angiotensin system than ACE inhibitors. (medscape.com)
These studies suggest that ACE inhibitors and/or angiotensin II receptor blockers may be effective treatments for diabetes and vascular and neural dysfunction. (diabetesjournals.org)
The beneficial effects of ACE inhibitors (ACEi) or angiotensin II type 1 receptor antagonists (AT 1 -ant) are reportedly mediated by NO in heart failure (HF). (ahajournals.org)
Current Guidelines for Using Angiotensin-Converting Enzyme Inhibitors and Angiotensin II-Receptor Antagonists in Chronic Kidney Disease: Is the Evidence Base Relevant to Older Adults? (annals.org)
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? (acpjc.org)
For patients with migraine headaches, I will continue to favor β-blockers followed by calcium channel blockers and perhaps angiotensin-converting enzyme inhibitors for prophylaxis, especially when comorbid hypertension exists. (acpjc.org)
While angiotensin-converting enzyme (ACE) inhibitors are established agents for the treatment of hypertension and heart failure, in contrast the angiotensin II receptor antagonists (AIIRAs) have failed to demonstrate more than equivalence in randomised clinical trials. (bjcardio.co.uk)
Angiotensin-Converting Enzyme Inhibitors and Angiotensin Receptor Blockers Modulate the Function of Myelinated Fibers after Chemotherapy: A Quantitative Sensory Testing Study. (semanticscholar.org)
Angiotensin II receptor antagonists work in a similar way to ACE inhibitors. (www.nhs.uk)
ADVERSE EFFECTS AND PRECAUTIONS Adverse effects of ACE inhibitors that result from inhibiting AngII-related functions also occur with ATJ receptor antagonists, including hypotension, hyperkalemia, and reduced renal function (especially associated with renal artery stenosis). (pharmacologicalsciences.us)
THERAPEUTIC USES When given in adequate doses, the ATj receptor antagonists appear to be as effective as ACE inhibitors in the treatment of hypertension. (pharmacologicalsciences.us)
Given their different mechanisms, there is no assurance that the effects of ACE inhibitors and antagonists of the ATj receptor will be equivalent in preventing target organ damage in patients with hypertension. (pharmacologicalsciences.us)
Synthesis and structure-activity relationships of a novel series of non-peptide angiotensin II receptor binding inhibitors specific for the AT2 subtype. (medchemexpress.com)
These agents are well-tolerated, with an incidence of adverse effects similar to that of placebo and significantly lower than experienced with the other class of renin-angiotensin system antagonists, the angiotensin-converting enzyme inhibitors. (elsevier.com)
Due to the fact that angiotensin II is without doubt one of the such a lot effective vasoconstrictors and a tremendous stimulus for the secretion of aldosterone from the adrenal gland, the improvement of of angiotensin II inhibitors is a vital step in regulating blood strain. (auroravietnamesecuisine.com)
ACE inhibitors block the conversion of Angiotensin I (ATI) to Angiotensin II (ATII). (wikipedia.org)
We specialize in small molecule inhibitors, agonists, antagonists and screening libraries! (apexbt.com)
Despite the huge amount of studies looking for candidate genes, the ACE gene remains the unique, well-characterized locus clearly associated with pathogenesis and progression of chronic kidney disease, and with response to treatment with drugs that directly interfere with the renin angiotensin system (RAS), such as angiotensin converting enzyme (ACE) inhibitors and angiotensin II receptor antagonists (ARA). (asnjournals.org)
Discussion: Angiotensin-converting enzyme inhibitors (ACEIs) and angiotensin receptor antagonists (ARAs) are among the most widely prescribed drugs for hypertension. (unifesp.br)
1 - 3 In many people with evidence of diabetic renal disease, however, angiotensin converting enzyme (ACE) inhibitors alone fail to achieve blood pressure targets. (bmj.com)
These antagonists, however, block only one subtype of the angiotensin II receptor, the type 1 subtype, and in contrast with ACE inhibitors do not promote accumulation of vasodilatory substances such as bradykinin. (bmj.com)
We analysed Medicare Australia Pharmaceutical Benefits Scheme claims for AHT drugs over the period 2004-2006, with special reference to the most prominent classes of AHT drugs currently used in Australia, namely angiotensin II receptor antagonists (A2RAs), angiotensin-converting enzyme inhibitors (ACEIs) and calcium channel blockers (CCBs). (mja.com.au)
They selectively block the activation of the AT1 receptor, preventing the binding of angiotensin II compared to ACE inhibitors. (wikipedia.org)

Two FDA officials are quarreling in public about their different views about the safety of angiotensin-receptor blockers (ARBs), according to a story by Thomas Burton in Friday's Wall Street Journal. (cardiobrief.org)
ARBs interfere with the binding of formed angiotensin II to its endogenous receptor. (medscape.com)
Although angiotensin receptor blockers (ARBs) are effective for patients with diabetes and chronic kidney disease in reducing or preventing cardiovascular diseases, there has been no decisive study that demonstrated treatment with ARBs is effective in patients on HD. (clinicaltrials.gov)
Angiotensin II receptor antagonists (ARBs, sartans) and breastfeeding. (e-lactancia.org)
What are angiotensin receptor blockers (ARBs) and how do they work? (xlx.pl)
Angiotensin II, through AT1 receptor stimulation, is a major stress hormone and, because (ARBs) block these receptors, in addition to their eliciting anti-hypertensive effects, may be considered for the treatment of stress-related disorders. (gutenberg.org)
Those patients taking angiotensin receptor blockers (ARBs) were 35-40% less likely to develop AD than those using other antihypertensives. (gutenberg.org)
This medication is angiotensin receptor blocker (ARBs), prescribed for hypertension. (medindia.net)
Angiotensin II receptor blockers (ARBs), formally angiotensin II receptor type 1 (AT1) antagonists, also known as angiotensin receptor blockers, angiotensin II receptor antagonists, or AT1 receptor antagonists, are a group of pharmaceuticals that bind to and inhibit the angiotensin II receptor type 1 (AT1) and thereby block the arteriolar contraction and sodium retention effects of renin-angiotensin system. (wikipedia.org)
Indeed, as a consequence of AT1 blockade, ARBs increase angiotensin II levels several-fold above baseline by uncoupling a negative-feedback loop. (wikipedia.org)

Clinical trials indicate that angiotensin-II receptor antagonists are effective and safe in the treatment of hypertension. (aafp.org)
Since the first angiotensin-II receptor antagonists were introduced a few years ago, numerous clinical trials have been conducted on their use in patients with hypertension and their potential use in patients with congestive heart failure. (aafp.org)
3 ) This article discusses the place of the newest class of antihypertensive agents, the angiotensin II receptor antagonists, in the treatment of hypertension. (aafp.org)
To treat hypertension, a class of Antihypertensive medications called "angiotensin II receptor antagonists" may be prescribed. (blausen.com)
receptor antagonist, on these complications of hypertension in stroke-prone spontaneously hypertensive rats (SHRSP) using Wistar Kyoto rats (WKY) as the control. (nii.ac.jp)
27 studies ( n = 12 110) that involved the use of angiotensin II receptor antagonists for treatment of mild-to-moderate hypertension (sitting diastolic blood pressure of 95 to 115 mm Hg) were included in the analysis. (acpjc.org)
I will use angiotensin II receptor antagonists as needed for hypertension control and hope that the hypothesis of this study is proven correct. (acpjc.org)
Concomitant use of PPAR-gamma agonists, thiazolidinediones, and angiotensin receptor blockers may be effective treatment for diabetes and hypertension. (journals.co.za)
Azilsartan medoxomil(TAK 491) is an orally administered angiotensin II receptor type 1 antagonist with IC50 of 0.62 nM, which used in the treatment of adults with essential hypertension. (medchemexpress.com)
Angiotensin II Receptor Blockers (ARB) and ARB Hypertension dosing. (xlx.pl)
The angiotensin II receptor antagonist candesartan cilexetil is widely used in the treatment of hypertension. (freethesaurus.com)
Decision Resources, one of the world's leading research and advisory firms for pharmaceutical and healthcare issues, finds that, owing primarily to the generic availability of the angiotensin II receptor antagonist (AIIRA) and the AIIRA/hydrochlorothiazide fixed dose combination (FDC) drug classes, the hypertension drug market will decline from approximately $26 billion in 2010 to $20. (freethesaurus.com)
President: Takakazu Morita) announced preliminary results of the overseas clinical trials of two drug candidates for lowering intraocular pressure in glaucoma and ocular hypertension: an angiotensin II receptor antagonist , DE-092 (INN: Olmesartan), and a prostaglandin derivative, DE-085 (INN: Tafluprost). (freethesaurus.com)
Boehringer Ingelheim and Yamanouchi also cooperate in Japan to co-promote MICARDIS(R) monotherapy (generic name telmisartan), an angiotensin II receptor antagonist discovered and developed by Boehringer Ingelheim for the treatment of hypertension. (freethesaurus.com)
In patients with mild-to-severe hypertension, the addition of an ATj receptor antagonist to a thiazide can produce significant additional reductions in blood pressure in patients who demonstrated an insufficient response to the first agent alone. (pharmacologicalsciences.us)
The angiotensin II type 1 receptor antagonists are the latest class of antihypertensive agents to be approved for treatment of hypertension. (elsevier.com)
An angiotensin-converting-enzyme inhibitor ( ACE inhibitor ) is a pharmaceutical drug used primarily for the treatment of hypertension (elevated blood pressure) and congestive heart failure . (wikipedia.org)
Navar and Rosivall showed that angiotensin II enhances the tone of the postglomerular arteriole ( 11 ), which induces glomerular hypertension and increases the filtration fraction ( 12 ), hemodynamic adaptations that in the long-term may cause glomerular damage and dysfunction ( 13 ). (asnjournals.org)
The COPE trial is planned to investigate, in patients with hypertension, which combination of the antihypertensive drugs, angiotensin receptor blockers, β-blockers or thiazide diuretics in addition to a long-acting calcium antagonist, benidipine hydrochloride, is superior to achieve the targeted blood pressure and prevent cardiovascular events with the fewest adverse drug effects. (clinicaltrials.gov)
This medication is an endothelin receptor antagonist, prescribed for pulmonary atrial hypertension (high blood pressure in the lungs). (medindia.net)
This medication is a dopamine receptor agonist, prescribed for severe hypertension. (medindia.net)
This medication is an angiotensin-converting enzyme inhibitor (ACE inhibitor), prescribed for high blood pressure (hypertension), congestive heart failure, myocardial infarction and kidney problems caused by diabetes. (medindia.net)
4 7 8 We compared the effects of candesartan 9 (a type 1 receptor blocker) and lisinopril 10 on blood pressure and urinary albumin excretion and evaluated the effects of the combination of both drugs in patients with hypertension, microalbuminuria, and type 2 diabetes. (bmj.com)

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)

Currently, they are considered reasonable alternatives for patients who have a compelling need for an angiotensin-converting enzyme (ACE) inhibitor but develop a cough while taking this medication. (aafp.org)
Adding a non-steroidal anti-inflammatory drug (NSAID) to dual antihypertensive therapy (a diuretic plus either an ACE inhibitor or an angiotensin receptor blocker) is associated with an increase in risk for kidney injury, according to a large new retrospective study published in BMJ. (cardiobrief.org)
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)
A type 1 receptor antagonist seems a reasonable alternative to an ACE inhibitor to maintain conduit vessel endothelial function in Type II diabetic subjects. (portlandpress.com)
The second drug (propranolol, a beta receptor antagonist), also functions as a monocyte migration inhibitor and as a TME modifying drug. (csuventures.org)
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)
This medication is an angiotensin-converting enzyme (ACE) inhibitor and thiazide diuretic combination, prescribed for high blood pressure. (medindia.net)
This medication is an angiotensin-converting enzyme (ACE) inhibitor, prescribed for high blood pressure. (medindia.net)
This medication is an ACE (angiotensin-converting enzyme) inhibitor, prescribed for high blood pressure either alone or with other medications. (medindia.net)
This medication is an angiotensin-converting enzyme (ACE) inhibitor, used alone or in combination with other medications to treat high blood pressure. (medindia.net)
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)

Kajiya T, Ho C, Wang J, Molecular and cellular effects of azilsartan: a new generation angiotensin II receptor blocker. (medchemexpress.com)
Only one randomized controlled trial compared the effects of an angiotensin 2 receptor antagonist with that of a calcium channel blocker in patients who had isolated Raynaud's or Raynaud's with systemic scleroderma . (sclerodermanews.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)

The effect of angiotensin-(1-7) was usually weaker than that of angiotensin II, and in contrast to angiotensin III the latencies were not significantly different. (nih.gov)
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)

Subtype 1 selective antagonists were effective at lower concentrations than selective subtype 2 antagonists. (nih.gov)
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)
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)
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)
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)
Olmesartan is a potent, competitive and selective Ang II type 1 receptor antagonist. (elsevier.com)

At this time, the place for the newest class of antihypertensive drugs, the angiotensin II receptor antagonists, remains uncertain. (aafp.org)
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)
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)
Antagonists of angiotensin II receptors, or blockers of AT1 receptors is one of the new groups of antihypertensive drugs. (otc-online-store.com)

The global Angiotensin Receptor Antagonists market is segmented by company, region (country), by Type, and by Application. (marketstudyreport.com)
Players, stakeholders, and other participants in the global Angiotensin Receptor Antagonists market will be able to gain the upper hand as they use the report as a powerful resource. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Market Size (US$ Million) by Region: 2016 VS 2021 &2027 Table 4. (marketstudyreport.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)

Olmesartan blocks the vasoconstrictor effects of angiotensin II by selectively blocking binding of angiotensin II to the AT-1 receptor in vascular smooth muscle. (medscape.com)
Olmesartan medoxomil is a new orally active angiotensin II (Ang II) type 1 receptor antagonist. (elsevier.com)
Yoshida, K & Kohzuki, M 2004, ' Clinical and experimental aspects of olmesartan medoxomil, a new angiotensin II receptor antagonist ', Cardiovascular Drug Reviews , vol. 22, no. 4, pp. 285-308. (elsevier.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)

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)
Whereas the excitatory effects of angiotensin-(1-7), angiotensin II and angiotensin III could always be inhibited with both angiotensin receptor subtype antagonists 1 and 2, that produced by angiotensin-(2-7) was only weakly antagonised, if at all. (nih.gov)
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)

Renin, an enzyme produced primarily by the juxtaglomerular cells of the kidney, catalyzes the conversion of angiotensinogen into an inactive substance, angiotensin I (A-I). Angiotensin-converting enzyme (ACE) then converts A-I to the physiologically active angiotensin II (A-II), which causes potent vasoconstriction, aldosterone secretion and sympathetic activation. (aafp.org)
This agent prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in lower aldosterone secretion. (medscape.com)
Enalapril prevents conversion of angiotensin I to angiotensin II, a potent vasoconstrictor, resulting in increased levels of plasma renin and a reduction in 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)

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)

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)
The aim of this study was to investigate the safety and efficacy of angiotensin II receptor type 1 antagonists (AT1RA) on hypertensive renal transplant recipients with proteinuria. (hippokratia.gr)

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)

Local angiotensin II promotes adipogenic differentiation of human adipose tissue mesenchymal stem cells through type 2 angiotensin receptor. (abcam.com)
The 35-day treatments of captopril and Dup 753 (angiotensin II type 1 receptor antagonist) significantly attenuated the increment of UAE levels (26.4% on dayl4 and 34.6% on day 28). (nii.ac.jp)
PD123177 (angiotensin II type 2 receptor antagonist) also attenuated the increment of UAE (24.7% on dayl4) at the dose of 150 mg/kg. (nii.ac.jp)
These results suggest that angiotensin II type 2 receptor as well as type 1 receptor may be involved in the development of diabetic nephropathy in the STZ-induced diabetic mice, and these mice are beneficial models of early diabetic nephropathy. (nii.ac.jp)
Together with the findings that both ACE inhibition and angiotensin II blockade improve resistance vessel function in this group, it is likely that at least some of the beneficial effect is mediated through the angiotensin II/type 1 receptor pathway. (portlandpress.com)
They also showed the down-regulation of atrial angiotensin II type 1 receptor (AT1R) and the up-regulation of AT2R in AF patients (2) . (onlinejacc.org)
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. (painresearchforum.org)
The angiotensin II type 2 receptor (AT2R) is a new target for neuropathic pain. (semanticscholar.org)
Global Angiotensin Receptor Antagonists Sales (US$ Million) Growth Rate by Type (2016 & 2021 & 2027) Table 2. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists by Company Type (Tier 1, Tier 2 and Tier 3) (based on the Revenue in Angiotensin Receptor Antagonists as of 2020) Table 17. (marketstudyreport.com)
Manufacturers Angiotensin Receptor Antagonists Product Type Table 20. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Sales (K Units) by Type (2016-2021) Table 22. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Revenue (US$ Million) Market Share by Type (2016-2021) Table 24. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Price (USD/Unit) by Type (2016-2021) Table 25. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Sales Share by Type (2022-2027) Table 26. (marketstudyreport.com)
Global Angiotensin Receptor Antagonists Price (USD/Unit) by Type (2022-2027) Table 29. (marketstudyreport.com)
Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR. (childrensmercy.org)
Functional reconstitution of the angiotensin II type 2 receptor and G(i) activation. (auroravietnamesecuisine.com)
4 - 6 The advent of angiotensin II type 1 (AT1) receptor blockers provides an alternative approach to blocking the renin-angiotensin system. (bmj.com)

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)

Nonpeptide angiotensin II receptor antagonist that blocks the vasoconstrictor and aldosterone-secreting effects of angiotensin II. (medscape.com)
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)

Although definitive evidence supporting dual blockade of the renin-angiotensin system has never been found, more than 200,000 patients in the US currently receive this therapy. (cardiobrief.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)

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)

Recent attention has focused on understanding the role of the brain-renin-angiotensin-system (RAS) in stroke and neurodegenerative diseases. (biomedcentral.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)

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)

The angiotensin II receptors , (AGTR1) and (AGTR2) , are a class of G protein-coupled receptors with angiotensin II as their ligands . (wikipedia.org)

Interaction of nonpeptide angiotensin II receptor antagonists with the urate transporter in rat renal brush-border membranes. (aspetjournals.org)

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)

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)
Some side effects of angiotensin 2 receptor antagonists include dizziness, localized tissue swelling, and increased levels of potassium in the blood ( hyperkalemia ). (sclerodermanews.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)

16. Stroth U, Blume A, Mielke K, Unger T. Angiotensin AT(2) receptor stimulates ERK1 and ERK2 in quiescent but inhibits ERK in NGF-stimulated PC12W cells. (exposurebiz.com)
Second, angiotensin II stimulates the release of antidiuretic hormone (ADH) and aldosterone, which increase the tubular reabsorption of sodium and free water, increasing the total circulating blood volume. (blausen.com)

These receptors are widespread in organs and tissues but are found predominately in vascular and myocardial tissue, the liver, the adrenal cortex (i.e., the zona glomerulosa tissue, which secretes aldosterone) and some areas of the brain. (aafp.org)
The authors concluded that Ang II-induced growth of vascular smooth muscle cells is mediated by AT 2 receptors, whereas the phenotypic changes of smooth muscle cells are AT 1 -dependent. (ahajournals.org)
The angiotensin (angio - vascular and tensio - a strain) - peptides produced in the body from angiotenzinoguena, which is a glycoprotein (ALPHA2-globulin) in blood plasma, which is synthesized in the liver. (otc-online-store.com)
The AT 2 receptor remains enigmatic and controversial - is probably involved in vascular growth. (wikipedia.org)

When data from ongoing trials become available, angiotensin II receptor antagonists may prove to be a good choice for initial therapy in many patients because of the favorable side effect profile of this class of drugs. (aafp.org)

Among other angiotensin receptor antagonists are TCV- 116, CV-11974, and CV-11194, all of which seem to be promising antihypertensives of the future. (ijpsonline.com)

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)

We investigated whether angiotensin II was involved with diabetic nephropathy in the mouse model. (nii.ac.jp)

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)
Angiotensin 2 binds to the angiotensin 2 receptors located on the muscular walls of blood vessels, causing the vessels to constrict. (sclerodermanews.com)

Whether RAS antagonists affect renal disease progression when intrarenal RAS activity is not increased is unclear. (asnjournals.org)

We also display that genetic or small molecule inhibition of the AHR results in the increased production of CD34+CD45+ HSPCs while conversely, activation of the same receptor results in a block of hematopoietic cell emergence. (shahmnil-mgh-harvard.org)
The role of inhibition of the renin-angiotensin system in preventing microvascular complications, particularly nephropathy, in patients with daibetes has been clearly shown. (bmj.com)

Under the influence of renin (an enzyme produced in juxtaglomerular apparatus of the kidney) polypeptide angiotensinogen non-Pressor activity, hydrolyses, forming angiotensin I is a biologically inactive Decapeptide, who are easily exposed to the further transformations. (otc-online-store.com)
Renin activates a circulating liver derived prohormone angiotensinogen by proteolytic cleavage of all but its first ten amino acid residues known as angiotensin I . ACE (Angiotensin converting enzyme) then removes a further two residues, converting angiotensin I into angiotensin II . (wikipedia.org)

Angiotensin II facilitates GABAergic neurotransmission at postsynaptic sites in rat amygdala neurons. (abcam.com)
This study explores the hypothesis that the renin-angiotensin system (RAS) is a potential target for preventing the loss of DA neurons. (biomedcentral.com)

Anatomy16

Organisms11

Diseases17

Chemicals and Drugs170

Analytical, Diagnostic and Therapeutic Techniques and Equipment21

Psychiatry and Psychology1

Phenomena and Processes23

Disciplines and Occupations1

Health Care5

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

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

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

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

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

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

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

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

Angiotensin Receptor Antagonists

Receptors, Angiotensin

Angiotensin II

Losartan

Tetrazoles

Angiotensin II Type 1 Receptor Blockers

Receptor, Angiotensin, Type 1

Biphenyl Compounds

Angiotensin-Converting Enzyme Inhibitors

Antihypertensive Agents

Imidazoles

Renin-Angiotensin System

Receptor, Angiotensin, Type 2

Angiotensin I

Hypertension

Blood Pressure

Angiotensin III

Benzimidazoles

Interleukin 1 Receptor Antagonist Protein

Angiotensin II Type 2 Receptor Blockers

Rats, Sprague-Dawley

Angiotensins

Neurokinin-1 Receptor Antagonists

Dose-Response Relationship, Drug

1-Sarcosine-8-Isoleucine Angiotensin II

Valine

Saralasin

Benzoates

Rats, Wistar

Peptidyl-Dipeptidase A

Renin

Pyridines

Purinergic P1 Receptor Antagonists

Kidney

Vasoconstrictor Agents

Histamine H2 Antagonists

Piperidines

Mineralocorticoid Receptor Antagonists

Serotonin 5-HT3 Receptor Antagonists

Excitatory Amino Acid Antagonists

Dopamine Antagonists

Serotonin 5-HT2 Receptor Antagonists

Hormone Antagonists

Adenosine A2 Receptor Antagonists

Drug Therapy, Combination

Fumarates

Aldosterone

Lisinopril

Receptors, Endothelin

Adenosine A1 Receptor Antagonists

Enalapril

Diuretics

Bradykinin

Purinergic P2 Receptor Antagonists

Cells, Cultured

Adrenergic beta-Antagonists

Benzazepines

Proteinuria

Narcotic Antagonists

Histamine H1 Antagonists

Amlodipine

Spironolactone

Angiotensinogen

Rats, Inbred SHR

Vasoconstriction

Disease Models, Animal

Time Factors

Muscarinic Antagonists

Heart Failure

Calcium Channel Blockers

RNA, Messenger

Receptor, Endothelin A

Ramipril

Hydrochlorothiazide

GABA-A Receptor Antagonists

Serotonin Antagonists

Histamine Antagonists

GABA Antagonists

Sialoglycoproteins

Muscle, Smooth, Vascular