Non-peptide AT2-receptor agonists

U Steckelings, Mats Larhed, Anders Hallberg, Robert Widdop, Emma Jones, Charlotta Wallinder, Pawel Namsolleck, Bjorn Dahlof, Thomas Unger

Research output: Contribution to journalArticleResearchpeer-review

84 Citations (Scopus)

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.
Original languageEnglish
Pages (from-to)187 - 192
Number of pages6
JournalCurrent Opinion in Pharmacology
Volume11
Issue number2
DOIs
Publication statusPublished - 2011

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