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Non-peptide AT2-receptor agonists
Center for Cardiovascular Research, Charité-Universitätsmedizin Berlin, Germany.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Pharmacy, Department of Medicinal Chemistry, Organic Pharmaceutical Chemistry.
Department of Pharmacology, Monash University, Clayton, Australia.
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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
Abstract [en]

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.
National Category
Pharmaceutical Sciences
Identifiers
URN: urn:nbn:se:uu:diva-153250DOI: 10.1016/j.coph.2010.11.002ISI: 000290127600014PubMedID: 21167778OAI: oai:DiVA.org:uu-153250DiVA: diva2:415737
Available from: 2011-05-09 Created: 2011-05-09 Last updated: 2017-12-11Bibliographically approved

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Larhed, MatsHallberg, AndersWallinder, Charlotta

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