Human beta(3) adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides

Authors
Naylor, EM Parmee, ER Colandrea, VJ Perkins, L Brockunier, L Candelore, MR Cascieri, MA Colwell, LF Deng, LP Feeney, WP Forrest, MJ Hom, GJ MacIntyre, DE Strader, CD Tota, L Wang, PR Wyvratt, MJ Fisher, MH Weber, AE
Citation
Em. Naylor et al., Human beta(3) adrenergic receptor agonists containing imidazolidinone and imidazolone benzenesulfonamides, BIOORG MED, 9(5), 1999, pp. 755-758
Citations number
6
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
5
Year of publication
1999
Pages
755 - 758
Database
ISI
SICI code
0960-894X(19990308)9:5<755:HBARAC>2.0.ZU;2-M
Abstract
The cyclopentylpropylimidazolidinone L-766,892 is a potent beta(3) AR agoni st (EC50 5.7 nM, 64% activation) with 420- and 130-fold selectivity over bi nding to the beta(1) and beta(2) ARs, respectively. In anesthetized rhesus monkeys, L-766,892 elicited dose-dependent hyperglycerolemia (ED50 0.1 mg/k g) with minimal effects on heart rate. (C) 1999 Elsevier Science Ltd. All r ights reserved.