| Literature DB >> 15537354 |
Yiqian Wan1, Charlotta Wallinder, Bianca Plouffe, Hélène Beaudry, A K Mahalingam, Xiongyu Wu, Berndt Johansson, Mathias Holm, Milad Botoros, Anders Karlén, Anders Pettersson, Fred Nyberg, Lars Fändriks, Nicole Gallo-Payet, Anders Hallberg, Mathias Alterman.
Abstract
The first druglike selective angiotensin II AT(2) receptor agonist (21) with a K(i) value of 0.4 nM for the AT(2) receptor and a K(i) > 10 microM for the AT(1) receptor is reported. Compound 21, with a bioavailability of 20-30% after oral administration and a half-life estimated to 4 h in rat, induces outgrowth of neurite cells, stimulates p42/p44(mapk), enhances in vivo duodenal alkaline secretion in Sprague-Dawley rats, and lowers the mean arterial blood pressure in anesthetized, spontaneously hypertensive rats. Thus, the peptidomimetic 21 exerts a similar biological response as the endogenous peptide angiotensin II after selective activation of the AT(2) receptor. Compound 21, derived from the prototype nonselective AT(1)/AT(2) receptor agonist L-162,313 will serve as a valuable research tool, enabling studies of the function of the AT(2) receptor in more detail.Entities:
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Year: 2004 PMID： 15537354 DOI： 10.1021/jm049715t
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446