Potent, selective benzenesulfonamide agonists of the human β3 adrenergic receptor
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.
Weber, Ann E.,Mathvink, Robert J.,Perkins, Leroy,Hutchins, Jennifer E.,Candelore, Mari R.,Tota, Laurie,Strader, Catherine D.,Wyvratt, Matthew J.,Fisher, Michael H.
p. 1101 - 1106
(2007/10/03)
More Articles about upstream products of 159182-38-4