Author/Authors :
Mark A. Ashwell، نويسنده , , William R. Solvibile Jr.، نويسنده , , Stella Han، نويسنده , , Elwood Largis، نويسنده , , Ruth Mulvey، نويسنده , , Jeffrey Tillet، نويسنده ,
Abstract :
The preparation and structure–activity relationships (SARs) of potent agonists of the human β3-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human β3-AR potency with selectivity over human β1-AR and/or human β2-AR agonism. Compound 29s was identified as a potent (EC50=1 nM) and selective (greater than 400-fold over β1- with no β2-AR agonism) full β3-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.
