title: Non-peptide AT2-receptor agonists.
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.
authors.affiliation: Center for Cardiovascular Research, Charité-Universitätsmedizin Berlin, Hessische Str. 3-4, 10115 Berlin, Germany. ulrike.steckelings@charite.de
authors.forename: U Muscha
authors.initials: UM
authors.lastname: Steckelings
authors.forename: Mats
authors.initials: M
authors.lastname: Larhed
authors.forename: Anders
authors.initials: A
authors.lastname: Hallberg
authors.forename: Robert E
authors.initials: RE
authors.lastname: Widdop
authors.forename: Emma S
authors.initials: ES
authors.lastname: Jones
authors.forename: Charlotta
authors.initials: C
authors.lastname: Wallinder
authors.forename: Pawel
authors.initials: P
authors.lastname: Namsolleck
authors.forename: Björn
authors.initials: B
authors.lastname: Dahlöf
authors.forename: Thomas
authors.initials: T
authors.lastname: Unger
mesh_terms: D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology; D001713:Biphenyl Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D001794:Blood Pressure / Q000187:drug effects; D015195:Drug Design; D006321:Heart / Q000187:drug effects; D006801:Humans; D007093:Imidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D007668:Kidney / Q000187:drug effects / Q000502:physiology; D044139:Receptor, Angiotensin, Type 2 / Q000819:agonists* / Q000502:physiology; D020521:Stroke / Q000517:prevention & control
chemical_list: D000893:Anti-Inflammatory Agents; D001713:Biphenyl Compounds; D007093:Imidazoles; C091630:L 162313; D044139:Receptor, Angiotensin, Type 2