Protein Information

Name AT1
Synonyms AG2S; AT1; AGTR 1; AGTR1; AGTR1A; AGTR1B; AT1AR; AT1B…

Compound Information

Name biphenyl
CAS 1,1′-biphenyl

Reference List

PubMed Abstract RScore(About this table)
18551021 Liu H, Kitazato KT, Uno M, Yagi K, Kanematsu Y, Tamura T, Tada Y, Kinouchi T, Nagahiro S: Protective mechanisms of the angiotensin II type 1 receptor blocker candesartan against cerebral ischemia: in-vivo and in-vitro studies. J Hypertens. 2008 Jul;26(7):1435-45.


BACKGROUND: Angiotensin II type 1 (AT1) receptor blockers decrease ischemia by mechanisms dependent on and independent of arterial blood pressure in hypertensive rats and AT1-R knockout mice, respectively.
3(0,0,0,3) Details
18300863 Ott C, Schlaich MP, Harazny J, Schmidt BM, Michelson G, Schmieder RE: Effects of angiotensin II type 1-receptor blockade on retinal endothelial function. J Hypertens. 2008 Mar;26(3):516-22.


Low-density lipoprotein-cholesterol may induce upregulation of angiotensin II type 1 (AT1)-receptors and their activation plays a pathogenetic role in atherosclerosis, possibly via enhanced breakdown of nitric oxide.
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18691848 Ohnuma Y, Toda M, Fujita M, Hosono K, Suzuki T, Ogawa Y, Amano H, Kitasato H, Hayakawa K, Majima M: Blockade of an angiotensin type I receptor enhances effects of radiation on tumor growth and tumor-associated angiogenesis by reducing vascular endothelial growth factor expression. Biomed Pharmacother. 2009 Feb;63(2):136-45. Epub 2007 Dec 26.


We had reported that Type 1 angiotensin receptor (AT1-R) antagonist reduced tumor-associated angiogenesis.
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19808375 Kassiri Z, Zhong J, Guo D, Basu R, Wang X, Liu PP, Scholey JW, Penninger JM, Oudit GY: Loss of angiotensin-converting enzyme 2 accelerates maladaptive left ventricular remodeling in response to myocardial infarction. Circ Heart Fail. 2009 Sep;2(5):446-55. Epub 2009 Jun 15.


Treatment of Ace2 (-)(/y)-MI mice with irbesartan, an AT1 receptor blocker, reduced nicotinamide-adenine dinucleotide phosphate oxidase activity, infarct size, MMP activation, and myocardial inflammation, ultimately resulting in improved post-MI ventricular function.
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18239590 Toblli JE, Munoz MC, Cao G, Mella J, Pereyra L, Mastai R: ACE inhibition and AT1 receptor blockade prevent fatty liver and fibrosis in obese Zucker rats. Obesity (Silver Spring). 2008 Apr;16(4):770-6. Epub 2007 Jan 24.

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19687342 Rossi GP: Losartan metabolite EXP3179: an AT1-receptor-independent treatment strategy for patients with the metabolic syndrome? Hypertension. 2009 Oct;54(4):710-2. Epub 2009 Aug 17.

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19016156 Sen S, Kanter M, Ustundag S, Aktas C, Dogutan H, Yalcin O: Effect of angiotensin-converting enzyme inhibition and angiotensin II type 1 receptor blockade on streptozotocin-induced diabetic nephropathy. Ren Fail. 2008;30(10):1023-33.


The aim of this study was designed to investigate the possible beneficial effects of the angiotensin-converting enzyme (ACE) inhibitor, Quinapril (Q) and, the angiotensin (ang) II T (1) (AT1) receptor blocker, irbesartan (Irb), in streptozotocin (STZ)-induced diabetes in rats.
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19230599 Kumar VV, Srinivas NR: Application of allometry principles for the prediction of human pharmacokinetic parameters for irbesartan, a AT1 receptor antagonist, from animal data. Eur J Drug Metab Pharmacokinet. 2008 Oct-Dec;33(4):247-52.

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19106212 Shweta A, Cullen-McEwen LA, Kett MM, Evans RG, Denton KM, Fitzgerald SM, Anderson WP, Bertram JF: Glomerular surface area is normalized in mice born with a nephron deficit: no role for AT1 receptors. Am J Physiol Renal Physiol. 2009 Mar;296(3):F583-9. Epub 2008 Dec 23.


An additional group of GDNF Het mice received the angiotensin type 1 (AT1)-receptor antagonist candesartan (Cand; 10 mg x kg (-1) x day (-1)) from 5 wk of age to determine the role of AT1 receptors in the compensatory hypertrophy.
1(0,0,0,1) Details
17959033 Liu BC, Xia HL, Wu JN, Zhang XL, Liu DG, Gong YX: Influence of irbesartan on expression of ILK and its relationship with epithelial-mesenchymal transition in mice with unilateral ureteral obstruction. Acta Pharmacol Sin. 2007 Nov;28(11):1810-8.


AIM: Irbesartan, a new antagonist of the type 1 angiotensin II receptor, has been proven to be renal protective in both diabetic and non-diabetic nephropathy, but its exact mechanism is still uncertain.
1(0,0,0,1) Details
18402243 Bramlage P, Schonrock E, Odoj P, Wolf WP, Funken C: [Importance of a fixed combination of AT1-receptor blockade and hydrochlorothiazide for blood pressure lowering in cardiac risk patients. MMW Fortschr Med. 2008 Jan 17;149 Suppl 4:172-81.

1(0,0,0,1) Details
19186482 : [Diastolic heart failure: AT1 blocker without effect] MMW Fortschr Med. 2008 Nov 20;150(47):13.

1(0,0,0,1) Details
19197922 Goebel M, Clemenz M, Staels B, Unger T, Kintscher U, Gust R: Characterization of new PPARgamma agonists: analysis of telmisartan's structural components. ChemMedChem. 2009 Mar;4(3):445-56.

In addition to a proven efficacy in lowering blood pressure, the AT1 receptor blocker telmisartan has recently been shown to exert pleiotropic effects as a partial agonist of the nuclear peroxisome proliferator-activated receptor gamma (PPARgamma).
The basic 1-(biphenyl-4-ylmethyl)-1H-benzimidazole scaffold of telmisartan was identified as an essential moiety with either a carboxylic acid or tetrazole group at the C-2 position of the biphenyl.
1(0,0,0,1) Details
18783396 Jing L, Li WM, Zhou LJ, Li S, Kou JJ, Song J: Expression of renin-angiotensin system and peroxisome proliferator-activated receptors in alcoholic cardiomyopathy. Alcohol Clin Exp Res. 2008 Nov;32(11):1999-2007. Epub 2008 Sep 9.


RESULTS: Compared with controls, myocardial angiotensin (Ang) I, Ang II, and renin levels were progressively increased at 2, 4, and 6 months of alcohol intake. mRNA expression of renin, angiotensinogen, angiotensin-converting enzyme (ACE), and AT1 was increased at 6 months.
1(0,0,0,1) Details
19560892 Sampath A, Reddy AR, Yakambaram B, Thirupathi A, Prabhakar M, Reddy PP, Reddy VP: Identification and characterization of potential impurities of valsartan, AT1 receptor antagonist. J Pharm Biomed Anal. 2009 Oct 15;50(3):405-12. Epub 2009 May 30.

Based on the spectral data (IR, NMR and MS) followed by synthesis, these impurities were characterized as (S)-N-(1-carboxy-2-methylprop-1-yl)-N-[2'-(1H-tetrazol-5-yl)-biphenyl-4-yl methyl] amine (impurity I); (S)-N-(1-carboxy-2-methylprop-1-yl)-N-(5-phenylthio) pentanoyl-N-[2'-(1H-te trazol-5-yl)-biphenyl-4-ylmethyl] amine (impurity II); (S)-N-(1-carboxy-2-methylprop-1-yl)-N-(5-phenyl) pentanoyl-N-[2'-(1H-tetraz ol-5-yl)-biphenyl-4-ylmethyl] amine (impurity III); (S)-N-(1-carboxy-2-methylprop-1-yl)-N-4-pentenoyl-N-[2'-(1H-tetrazol-5-yl) -biphenyl-4-ylmethyl] amine (impurity IV); (S)-N-(1-carboxy-2-methylprop-1-yl)-N-(5-hydroxy) pentanoyl-N-[2'-(1H-tetra zol-5-yl)-biphenyl-4-ylmethyl] amine (impurity V).
1(0,0,0,1) Details
19348247 Kim-Mitsuyama S: [Pharmacological characteristics of ARB and potential strategy to develop novel ARB]. Nippon Rinsho. 2009 Apr;67(4):812-8.


Six AT1 receptor blockers (ARBs) are clinically available in Japan.
1(0,0,0,1) Details
19445841 Ozdemir S, Tandogan B, Ulusu NN, Turan B: Angiotensin II receptor blockage prevents diabetes-induced oxidative damage in rat heart. Folia Biol. 2009;55(1):11-6.


In this study we aimed to investigate the effect of angiotensin II type 1 (AT1) receptor blockage on some antioxidant enzymes such as glucose- 6-phosphate dehydrogenase (G6PD), 6-phoshogluconate dehydrogenase (6PGD), glutathione reductase (GR), glutathione-S-transferase (GST), glutathione peroxidase (GSH-Px), and catalase (CAT) in the heart of streptozotocin (STZ)-induced diabetic rats.
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