BMS-196085: A potent and selective full agonist of the human beta(3) adrenergic receptor

Authors
Gavai, AV Sher, PM Mikkilineni, AB Poss, KM McCann, PJ Girotra, RN Fisher, LG Wu, G Bednarz, MS Mathur, A Wang, TC Sun, CQ Slusarchyk, DA Skwish, S Allen, GT Hillyer, DE Frohlich, BH Abboa-Offei, BE Cap, M Waldron, TL George, RJ Tesfamariam, B Harper, TW Ciosek, CP Young, DA Dickinson, KE Seymour, AA Arbeeny, CM Washburn, WN
Citation
Av. Gavai et al., BMS-196085: A potent and selective full agonist of the human beta(3) adrenergic receptor, BIOORG MED, 11(23), 2001, pp. 3041-3044
Citations number
16
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
23
Year of publication
2001
Pages
3041 - 3044
Database
ISI
SICI code
0960-894X(200112)11:23<3041:BAPASF>2.0.ZU;2-U
Abstract
A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prep ared and evaluated for their human beta (3) adrenergic receptor agonist act ivity. SAR studies led to the identification of BMS-196085 (25), a potent b eta (3) full agonist (K-i = 21 nM, 95% activation) with partial agonist (45 %) activity at the beta (1) receptor. Based on its desirable in vitro and i n vivo properties, BMS-196085 was chosen for clinical evaluation. (C) 2001 Elsevier Science Ltd. All rights reserved.