Author/Authors :
Ann E. Weber، نويسنده , , Robert J. Mathvink، نويسنده , , Leroy Perkins، نويسنده , , Jennifer E. Hutchins، نويسنده , , Mari R. Candelore، نويسنده , , Laurie Tota، نويسنده , , Catherine D. Strader، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Michael H. Fisher، نويسنده ,
Abstract :
A cloned human β3 adrenergic receptor assay was used to identify phenoxypropanolamine agonist 1. SAR studies led to the identification of benzenesulfonamide derivative 20, a 6.3 nM β3 agonist which shows 30-fold selectivity for β3 agonist activity over β1 and β2 receptor binding. Further refinement of this lead provided 4-bromo derivative 39, a subnanomolar agonist with 660-fold and 230-fold selectivity over β1 and β2, respectively.
