BMS-196085: A potent and selective full agonist of the human β3 adrenergic receptor

Abstract A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human β 3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-196085 ( 25 ), a potent β 3 full agonist ( K i =21 nM, 95% activation) with partial agonist (45%) activity at the β 1 receptor. Based on its desirable in vitro and in vivo properties, BMS-196085 was chosen for clinical evaluation.