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The past, present and future of angiotensin II type 2 receptor stimulation

Item Type:Article
Title:The past, present and future of angiotensin II type 2 receptor stimulation
Creators Name:Steckelings, U.M. and Rompe, F. and Kaschina, E. and Namsolleck, P. and Grzesiak, A. and Funke-Kaiser, H. and Bader, M. and Unger, T.
Abstract:Studying the angiotensin type 2 receptor (AT2) has been problematic in the past because a pharmacological tool for direct, specific in vitro and in vivo stimulation of the receptor has been lacking. Consequently, current knowledge about AT2 receptor signalling and function had to be obtained by indirect approaches, like studying animals or cells with genetically altered AT2 receptor expression levels, inhibitory experiments using specific AT2 receptor antagonists, stimulation with angiotensin II under concomitant angiotensin II type 1 receptor blockade or stimulation with the peptide agonist CGP42112A, which has additional AT2 receptor antagonistic properties. The recently developed non-peptide AT2 receptor agonist Compound 21 now, for the first time, allows direct, selective and specific AT2 receptor stimulation in vitro and in vivo. This new tool will certainly revolutionise AT2 receptor research, enable many new insights into AT2 receptor function and may also have the potential to become a future medical drug. This article reviews milestone findings about AT2 receptor functional properties obtained by 'conventional' experimental approaches within the last 20 years. Moreover, it provides an overview of the first results obtained by direct AT2 receptor stimulation with Compound 21, comprising effects on alkaline secretion, neurite outgrowth, blood pressure and post-infarct cardiac function.
Keywords:Angiotensin, AT2 Receptor, AT2 Receptor Stimulation, Drug Development, Myocardial Infarction, Animals
Source:Journal of the Renin Angiotensin Aldosterone System
Page Range:67-73
Date:March 2010
Official Publication:https://doi.org/10.1177/1470320309347791
PubMed:View item in PubMed

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