Human beta(3) adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides

Authors
Parmee, ER Naylor, EM Perkins, L Colandrea, VJ Ok, HO Candelore, MR Cascieri, MA 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
Er. Parmee et al., Human beta(3) adrenergic receptor agonists containing cyclic ureidobenzenesulfonamides, BIOORG MED, 9(5), 1999, pp. 749-754
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
749 - 754
Database
ISI
SICI code
0960-894X(19990308)9:5<749:HBARAC>2.0.ZU;2-L
Abstract
Human beta(3) adrenergic receptor agonists containing 5-membered ring ureas were shown to be potent partial agonists with excellent selectivity over b eta(1) and beta(2) binding. L-760,087 (4a) and L-764,646 (5a) (beta(3) EC50 = 18 and 14 nM, respectively) stimulate lipolysis in rhesus monkeys (ED50 = 0.2 and 0.1 mg/kg, respectively) with minimal effects on heart rate. Oral absorption in dogs is improved over other urea analogs. (C) 1999 Elsevier Science Ltd. All rights reserved.