L-770,644: A potent and selective human beta(3) adrenergic receptor agonist with improved oral bioavailability

Authors
Shih, TL Candelore, MR Cascieri, MA Chiu, SHL Colwell, LF Deng, LP Feeney, WP Forrest, MJ Hom, GJ MacIntyre, DE Miller, RR Stearns, RA Strader, CD Tota, L Wyvratt, MJ Fisher, MH Weber, AE
Citation
Tl. Shih et al., L-770,644: A potent and selective human beta(3) adrenergic receptor agonist with improved oral bioavailability, BIOORG MED, 9(9), 1999, pp. 1251-1254
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
9
Year of publication
1999
Pages
1251 - 1254
Database
ISI
SICI code
0960-894X(19990503)9:9<1251:LAPASH>2.0.ZU;2-9
Abstract
L-770,644 (9c) is a potent and selective agonist of the human pg adrenergic receptor (EC50 = 13 nM). It shows good oral bioavailability in both dogs a nd rats (%F = 27), and is a full agonist for glycerolemia in the rhesus mon key (ED50 = 0.21 mg/kg). Based on its desirable in vitro and in vivo proper ties, L-770,644 was chosen for further preclinical evaluation. (C) 1999 Els evier Science Ltd. All rights reserved.