Non-peptide AT2-receptor agonists
2011 (English)In: Current opinion in pharmacology (Print), ISSN 1471-4892, E-ISSN 1471-4973, Vol. 11, no 2, 187-192 p.Article in journal (Refereed) Published
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.
Place, publisher, year, edition, pages
2011. Vol. 11, no 2, 187-192 p.
IdentifiersURN: urn:nbn:se:uu:diva-153250DOI: 10.1016/j.coph.2010.11.002ISI: 000290127600014PubMedID: 21167778OAI: oai:DiVA.org:uu-153250DiVA: diva2:415737