Target type: molecularfunction
An angiotensin receptor activity that acts via Gq-mediated activation of phospholipase C followed by phosphoinositide hydrolysis and Ca2+ signaling, and may act via additional signaling mechanisms. [GOC:mah, PMID:10977869]
Angiotensin type 1 receptor (AT1R) activity is a molecular function that plays a crucial role in regulating blood pressure and electrolyte balance. AT1R is a G protein-coupled receptor (GPCR) that is activated by angiotensin II (AngII), a potent vasoconstrictor peptide. Upon binding of AngII to AT1R, a conformational change occurs in the receptor, triggering a cascade of downstream signaling events.
The activation of AT1R leads to the activation of various intracellular signaling pathways, including the mitogen-activated protein kinase (MAPK) pathway, the phospholipase C (PLC) pathway, and the phosphoinositide 3-kinase (PI3K) pathway. These signaling pathways ultimately result in a variety of physiological responses, including vasoconstriction, aldosterone release, sodium reabsorption, and cell growth.
Specifically, AT1R activation leads to:
* **Vasoconstriction:** AngII binding to AT1R stimulates the release of calcium ions from intracellular stores, leading to smooth muscle contraction and vasoconstriction. This contributes to the increase in blood pressure mediated by AngII.
* **Aldosterone release:** AT1R activation in the adrenal glands triggers the synthesis and release of aldosterone, a hormone that promotes sodium reabsorption and potassium excretion by the kidneys. This contributes to the regulation of blood volume and electrolyte balance.
* **Sodium reabsorption:** AT1R activation in the kidneys promotes sodium reabsorption, which in turn leads to water retention and increased blood volume.
* **Cell growth:** AT1R activation can also stimulate cell growth and proliferation, contributing to the development of cardiovascular disease.
Overall, angiotensin type 1 receptor activity is a complex and multifaceted process that plays a crucial role in the regulation of blood pressure, electrolyte balance, and cardiovascular function. Its dysregulation is associated with various pathological conditions, including hypertension, heart failure, and kidney disease.'
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| Protein | Definition | Taxonomy |
|---|---|---|
| Type-1 angiotensin II receptor | An angiotensin II receptor 1 that is encoded in the genome of cow. [OMA:P25104, PRO:DNx] | Bos taurus (cattle) |
| Type-1 angiotensin II receptor | An angiotensin II receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P30556] | Homo sapiens (human) |
| Compound | Definition | Classes | Roles |
|---|---|---|---|
| 5-iodo-2-(oxaloamino)benzoic acid | organoiodine compound | ||
| candesartan | candesartan : A benzimidazolecarboxylic acid that is 1H-benzimidazole-7-carboxylic acid substituted by an ethoxy group at position 2 and a ({2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl}methyl) group at position 1. It is a angiotensin receptor antagonist used for the treatment of hypertension. candesartan: a nonpeptide angiotensin II receptor antagonist | benzimidazolecarboxylic acid; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| thiorphan | Thiorphan: A potent inhibitor of membrane metalloendopeptidase (ENKEPHALINASE). Thiorphan potentiates morphine-induced ANALGESIA and attenuates naloxone-precipitated withdrawal symptoms. | N-acyl-amino acid | |
| avapro | irbesartan : A biphenylyltetrazole that is an angiotensin II receptor antagonist used mainly for the treatment of hypertension. Irbesartan: A spiro compound, biphenyl and tetrazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION, and in the treatment of kidney disease. | azaspiro compound; biphenylyltetrazole | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| losartan | losartan : A biphenylyltetrazole where a 1,1'-biphenyl group is attached at the 5-position and has an additional trisubstituted imidazol-1-ylmethyl group at the 4'-position Losartan: An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II. | biphenylyltetrazole; imidazoles | angiotensin receptor antagonist; anti-arrhythmia drug; antihypertensive agent; endothelin receptor antagonist |
| propranolol | propranolol : A propanolamine that is propan-2-ol substituted by a propan-2-ylamino group at position 1 and a naphthalen-1-yloxy group at position 3. Propranolol: A widely used non-cardioselective beta-adrenergic antagonist. Propranolol has been used for MYOCARDIAL INFARCTION; ARRHYTHMIA; ANGINA PECTORIS; HYPERTENSION; HYPERTHYROIDISM; MIGRAINE; PHEOCHROMOCYTOMA; and ANXIETY but adverse effects instigate replacement by newer drugs. | naphthalenes; propanolamine; secondary amine | anti-arrhythmia drug; antihypertensive agent; anxiolytic drug; beta-adrenergic antagonist; environmental contaminant; human blood serum metabolite; vasodilator agent; xenobiotic |
| atomoxetine | atomoxetine : A secondary amino compound having methyl and 3-(2-methylphenoxy)-3-phenylpropan-1-yl substituents. | aromatic ether; secondary amino compound; toluenes | adrenergic uptake inhibitor; antidepressant; environmental contaminant; xenobiotic |
| ipsapirone | N-arylpiperazine | ||
| flesinoxan | |||
| valsartan | valsartan : A monocarboxylic acid amide consisting of L-valine in which the amino hydrogens have been replaced by a pentanoyl and a [2'-(1H-tetrazol-5-yl)biphenyl]-4-yl]methyl group. It exhibits antihypertensive activity. Valsartan: A tetrazole derivative and ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKER that is used to treat HYPERTENSION. | biphenylyltetrazole; monocarboxylic acid; monocarboxylic acid amide | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| tasosartan | tasosartan: angiotensin II antagonist; structure given in first source | biphenyls | |
| telmisartan | telmisartan : A member of the class of benzimidazoles used widely in the treatment of hypertension. Telmisartan: A biphenyl compound and benzimidazole derivative that acts as an angiotensin II type 1 receptor antagonist. It is used in the management of HYPERTENSION. | benzimidazoles; biphenyls; carboxybiphenyl | angiotensin receptor antagonist; antihypertensive agent; EC 3.4.15.1 (peptidyl-dipeptidase A) inhibitor; environmental contaminant; xenobiotic |
| gr 117289 | GR 117289: angiotensin AT1 receptor antagonist; structure given in first source zolasartan : A member of the class of 1-benzofurans that is 3-bromo-1-benzofuran which is substituted by a 2-(1H-tetrazol-5-yl)phenyl group at position 2 and by a (2-butyl-5-carboxy-4-chloro-1H-imidazol-1-yl)methyl group at position 5. It is an angiotensin II receptor type 1 (AT1) antagonist and was in clinical trials for the treatment of hypertension (now discontinued). | 1-benzofurans; biaryl; imidazolyl carboxylic acid; monocarboxylic acid; organobromine compound; organochlorine compound; tetrazoles | angiotensin receptor antagonist; antihypertensive agent |
| exp3174 | losartan carboxylic acid : A biphenylyltetrazole that is losartan with the hydroxymethyl group at position 5 on the imidazole ring replaced with a carboxylic acid. losartan carboxylic acid: structure given in first source | biphenylyltetrazole; imidazoles; organochlorine compound | metabolite |
| l 692429 | L 692429: stimulates release of growth hormone; RN refers to (R)-isomer; structure given in first source | ||
| angiotensin ii, des-asp(1)-des-arg(2)-ile(5)- | angiotensin II, des-Asp(1)-des-Arg(2)-Ile(5)-: 3-8 hexapeptide fragment of angiotensin II; smallest potent angiotensin II antagonist | organic molecular entity | |
| exp7711 | EXP7711: to search, use E#P7711(nm); angiotensin II receptor antagonist; structure given in first source | ||
| bibs 39 | BIBS 39: structure given in first source; angiotensin II receptor antagonist | ||
| bibs 222 | BIBS 222: structure given in first source; angiotensin II receptor antagonist | ||
| forasartan | forasartan : A member of the class of pyridines that is pyridine which is substituted at positions 2 and 5 by o-(tetrazol-5-yl)phenyl and (3,5-dibutyl-1,2,4-triazol-1-yl)methyl groups, respectively. It is a nonpeptide antagonist of angiotensin II, type 1 (AT1) receptors, used for the treatment of hypertension. forasartan: structure given in first source; an angiotensin AT(1) receptor antagonist; angiotensin II receptor antagonist; used in treatment of congestive heart failure | benzenes; pyridines; tetrazoles; triazoles | angiotensin receptor antagonist; antihypertensive agent |
| up 269-6 | UP 269-6: structure given in first source; angiotensin receptor antagonist | ||
| mk 996 | MK 996: an AT1-selective angiotensin II receptor antagonist; structure given in first source | ||
| bms 207940 | N-((2'-(((4,5-dimethyl-3-isoxazolyl)amino)sulfonyl)-4-(2-oxazolyl)(1,1'-biphenyl)-2-yl)methyl)-N,3,3-trimethylbutanamide: an ET(A) receptor antagonist; structure in first source | ||
| angiotensin ii | Giapreza: injectable form of angiotensin II used to increase blood pressure in adult patients with septic or other distributive shock Ile(5)-angiotensin II : An angiotensin II that acts on the central nervous system (PDB entry: 1N9V). | amino acid zwitterion; angiotensin II | human metabolite |
| piboserod | Serotonin 5-HT4 Receptor Antagonists: Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS. | ||
| l 158809 | L 158809: RN & structure given in first source; angiotensin receptor antagonist | ||
| 2-(oxaloamino)benzoic acid | (oxaloamino)benzoic acid | ||
| omapatrilat | omapatrilat: structure in first source | dipeptide | |
| caffeic acid | trans-caffeic acid : The trans-isomer of caffeic acid. | caffeic acid | geroprotector; mouse metabolite |
| cv 11194 | CV 11194: structure given in first source; an angiotensin II receptor antagonist | ||
| milfasartan | milfasartan: angiotensin I receptor antagonist; structure in first source | ||
| eprosartan | eprosartan : A member of the class of imidazoles and thiophenes that is an angiotensin II receptor antagonist used for the treatment of high blood pressure. eprosartan: angiotensin II receptor antagonist | dicarboxylic acid; imidazoles; thiophenes | angiotensin receptor antagonist; antihypertensive agent; environmental contaminant; xenobiotic |
| pd 123319 | PD123319 : An imidazopyridine consisting of 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine having 4-(dimethylamino)-3-methylbenzyl, diphenylacetyl and carboxy and groups at positions 1, 5 and 6 respectively | imidazopyridine | angiotensin receptor antagonist; endothelin receptor antagonist; vasoconstrictor agent |
| exp 655 | |||
| angiotensin ii, 1-sar-5-ile-8-ala- | |||
| saralasin | Saralasin: 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. | oligopeptide | |
| l 162313 | L 162313: a biphenylimidazole derivative; a non-peptide angiotensin agonist; no further information available 2/95 | ||
| 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4h-pyran-3-yl 4-nitrobenzoate | 4-oxo-6-((pyrimidin-2-ylthio)methyl)-4H-pyran-3-yl 4-nitrobenzoate: structure in first source | nitrobenzoic acid | |
| zd 7155 | |||
| bms 193884 | |||
| l 163491 | L 163491: structure given in first source | ||
| fimasartan | fimasartan: an angiotensin II receptor antagonist | biphenyls | |
| bms 248360 | |||
| ema401 | |||
| naluzotan | naluzotan: an antidepressant and anti-anxiety agent; structure in first source | ||
| nitd 609 | NITD 609: an antimalarial and coccidiostat; structure in first source |