TY - JOUR
AU - Alterman, Mathias
AB - 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.
TI - Design, synthesis, and biological evaluation of the first selective nonpeptide AT2 receptor agonist.
JF - Journal of Medicinal Chemistry
DO - 10.1021/jm049715t
DA - 2005-01-03
UR - https://www.deepdyve.com/lp/pubmed/design-synthesis-and-biological-evaluation-of-the-first-selective-91GoyF3sEi
SP - 5995
EP - 6008
VL - 47
IS - 24
DP - DeepDyve
ER -