期刊
CURRENT OPINION IN PHARMACOLOGY
卷 11, 期 2, 页码 187-192出版社
ELSEVIER SCI LTD
DOI: 10.1016/j.coph.2010.11.002
关键词
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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 021 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. 021 is awaited to enter a phase I clinical study in 2011.
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