Document Report Card

Basic Information

ID: ALA1133858

Journal: Bioorg Med Chem Lett

Title: 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.

Abstract: A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 (25), a potent beta(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 in vivo properties, BMS-196085 was chosen for clinical evaluation.

CiteXplore: 11714606

DOI: 10.1016/s0960-894x(01)00629-1