Literature DB >> 14998339

First reported nonpeptide AT1 receptor agonist (L-162,313) acts as an AT2 receptor agonist in vivo.

Yiqian Wan1, Charlotta Wallinder, Berndt Johansson, Mathias Holm, A K Mahalingam, Xiongyu Wu, Milad Botros, Anders Karlén, Anders Pettersson, Fred Nyberg, Lars Fändriks, Anders Hallberg, Mathias Alterman.   

Abstract

In this investigation, it is demonstrated that the first nonpeptide AT(1) receptor agonist L-162,313 (1), disclosed in 1994, also acts as an agonist at the AT(2) receptor. In anesthetized rats, administration of compound 1 intravenously or locally in the duodenum increased duodenal mucosal alkaline secretion, effects that were sensitive to the selective AT(2) receptor antagonist PD-123,319. The data strongly suggest that 1 is an AT(2) receptor agonist in vivo. To the best of our knowledge, this substance is the first nonpeptidic low-molecular weight compound with an agonistic effect mediated through the AT(2) receptor.

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Year:  2004        PMID: 14998339     DOI: 10.1021/jm031031i

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  6 in total

1.  The Protective Effects of Compound 21 and Valsartan in Isoproterenol-Induced Myocardial Injury in Rats.

Authors:  Zeynep Ulutas; Necip Ermis; Onural Ozhan; Hakan Parlakpinar; Nigar Vardi; Burhan Ates; Cemil Colak
Journal:  Cardiovasc Toxicol       Date:  2020-07-09       Impact factor: 3.231

2.  Enhanced Natriuresis and Diuresis in Wistar Rats Caused by the Costimulation of Renal Dopamine D3 and Angiotensin II Type 2 Receptors.

Authors:  Sufei Yang; Yu Han; Shuo Zheng; Xun Kou; Laureano D Asico; Hefei Huang; Zhao Gao; Pedro A Jose; Chunyu Zeng
Journal:  Am J Hypertens       Date:  2015-03-13       Impact factor: 2.689

3.  Stimulation of angiotensin AT2 receptors by the non-peptide agonist, Compound 21, evokes vasodepressor effects in conscious spontaneously hypertensive rats.

Authors:  S Bosnyak; I K Welungoda; A Hallberg; M Alterman; R E Widdop; E S Jones
Journal:  Br J Pharmacol       Date:  2010-01-28       Impact factor: 8.739

Review 4.  The Angiotensin AT2 Receptor: From a Binding Site to a Novel Therapeutic Target.

Authors:  U Muscha Steckelings; Robert E Widdop; Edward D Sturrock; Lizelle Lubbe; Tahir Hussain; Elena Kaschina; Thomas Unger; Anders Hallberg; Robert M Carey; Colin Sumners
Journal:  Pharmacol Rev       Date:  2022-10       Impact factor: 18.923

Review 5.  AT2 receptors: functional relevance in cardiovascular disease.

Authors:  Emma S Jones; Antony Vinh; Claudia A McCarthy; Tracey A Gaspari; Robert E Widdop
Journal:  Pharmacol Ther       Date:  2008-08-31       Impact factor: 12.310

6.  N-Aryl Isoleucine Derivatives as Angiotensin II AT2 Receptor Ligands.

Authors:  Malte Behrends; Charlotta Wallinder; Anna Wieckowska; Marie-Odile Guimond; Anders Hallberg; Nicole Gallo-Payet; Mats Larhed
Journal:  ChemistryOpen       Date:  2014-03-13       Impact factor: 2.911

  6 in total

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