Target type: molecularfunction
An angiotensin receptor activity that acts via Gi protein coupling and cGMP (NO) generation, and may also act via additional signaling mechanisms. [GOC:mah, PMID:10977869]
Angiotensin type II receptor activity is a molecular function associated with the angiotensin II receptor (AT2R), a G protein-coupled receptor (GPCR) that binds to angiotensin II (Ang II). Ang II is a potent vasoconstrictor and aldosterone-stimulating hormone, playing a central role in regulating blood pressure and electrolyte balance. AT2R activation initiates a signaling cascade involving G proteins, leading to diverse cellular responses. These responses are often counter-regulatory to the effects of AT1R, the other major angiotensin II receptor. Key aspects of AT2R activity include:
1. **Signal Transduction:** Upon Ang II binding, AT2R activates intracellular signaling pathways, primarily through coupling with G proteins, particularly Gq and Gi/o proteins. Gq activation triggers phospholipase C (PLC) signaling, leading to an increase in intracellular calcium levels and activation of protein kinase C (PKC). Gi/o activation inhibits adenylyl cyclase activity, leading to a decrease in cAMP levels.
2. **Vascular Effects:** Unlike AT1R, AT2R activation generally elicits vasodilatory effects. This vasodilation is mediated through various mechanisms, including nitric oxide (NO) production, modulation of vascular smooth muscle cell contractility, and suppression of reactive oxygen species (ROS) production.
3. **Cardiovascular Protection:** Studies have demonstrated that AT2R activation exerts protective effects on the cardiovascular system. It has been shown to attenuate cardiac hypertrophy, fibrosis, and apoptosis, contributing to improved cardiac function and reduced risk of heart failure.
4. **Renal Function Regulation:** AT2R activity plays a role in regulating renal function, potentially influencing processes such as sodium and water reabsorption, and promoting diuresis.
5. **Neurological Effects:** AT2R activation has been implicated in neurological functions, including modulation of neuronal excitability, neuroprotection, and cognitive function.
6. **Endocrine Effects:** AT2R activity may influence endocrine function, particularly in regulating aldosterone synthesis and release, contributing to electrolyte balance.
7. **Developmental Roles:** AT2R has been implicated in various developmental processes, including embryonic development and tissue regeneration.
The specific molecular function of AT2R activity is complex and multifaceted, involving a wide range of signaling pathways and cellular responses. Its role in regulating cardiovascular function, promoting vasodilation, and exerting protective effects on the heart and other organs makes it a potential therapeutic target for various cardiovascular diseases and other disorders.'
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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-2 angiotensin II receptor | An angiotensin II receptor 2 that is encoded in the genome of human. [PRO:WCB, UniProtKB:P50052] | Homo sapiens (human) |
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) |
Proto-oncogene Mas | A G-protein coupled receptor MAS that is encoded in the genome of human. [PRO:WCB, UniProtKB:P04201] | 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 |
miconazole | 1-[2-(2,4-dichlorobenzyloxy)-2-(2,4-dichlorophenyl)ethyl]imidazole : A member of the class of imidazoles that is 1-(2,4-dichlorophenyl)-2-(imidazol-1-yl)ethanol in which the hydroxyl hydrogen is replaced by a 2,4-dichlorobenzyl group. miconazole : A racemate composed of equimolar amounts of (R)- and (S)-miconazole. Used (as its nitrate salt) to treat skin infections such as athlete's foot, jock itch, ringworm and other fungal skin infections. It inhibits the synthesis of ergosterol, a critical component of fungal cell membranes. Miconazole: An imidazole antifungal agent that is used topically and by intravenous infusion. | dichlorobenzene; ether; imidazoles | |
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 |
bexarotene | benzoic acids; naphthalenes; retinoid | antineoplastic 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 | ||
a 81988 | A 81988: angiotensin II antagonist selective for type 1 receptors | ||
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 | ||
chrysamine g | chrysamine G: structure given in first source; RN refers to disodium salt | ||
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 | ||
alitretinoin | Alitretinoin: A retinoid that is used for the treatment of chronic hand ECZEMA unresponsive to topical CORTICOSTEROIDS. It is also used to treat cutaneous lesions associated with AIDS-related KAPOSI SARCOMA. | retinoic acid | antineoplastic agent; keratolytic drug; metabolite; retinoid X receptor agonist |
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 | ||
tak 013 | |||
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 | |||
ave 0991 | AVE 0991: structure in first source | ||
l 163491 | L 163491: structure given in first source | ||
nrx 194204 | IRX4204: retinoid X receptor (RXR) agonist; structure in first source | ||
agn 194204 | AGN 194204: a retinoid X receptor ligand; structure 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 |