Non-peptide AT2-receptor agonists.

Curr Opin Pharmacol 2011 Apr 15;11(2):187-92. Epub 2010 Dec 15.

Center for Cardiovascular Research, Charité-Universitätsmedizin Berlin, Hessische Str. 3-4, 10115 Berlin, Germany.

The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after myocardial infarction and in hypertension-induced end organ damage, notably in a blood-pressure independent way. In all of these models, AT2-receptor mediated anti-inflammation seemed an important underlying mechanism. C21 is awaited to enter a phase I clinical study in 2011.

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http://dx.doi.org/10.1016/j.coph.2010.11.002DOI Listing
April 2011
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