| Literature DB >> 21167778 |
U Muscha Steckelings1, Mats Larhed, Anders Hallberg, Robert E Widdop, Emma S Jones, Charlotta Wallinder, Pawel Namsolleck, Björn Dahlöf, Thomas Unger.
Abstract
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.Entities:
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Year: 2010 PMID： 21167778 DOI： 10.1016/j.coph.2010.11.002
Source DB: PubMed Journal: Curr Opin Pharmacol ISSN： 1471-4892 Impact factor: 5.547