Author/Authors :
Emma R. Parmee، نويسنده , , Linda L. Brockunier، نويسنده , , Jiafang He، نويسنده , , Suresh B. Singh، نويسنده , , Mari R. Candelore، نويسنده , , Margaret A. Cascieri، نويسنده , , Liping Deng، نويسنده , , Yong Liu، نويسنده , , Laurie Tota، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Michael H. Fisher، نويسنده , , Ann E. Weber، نويسنده ,
Abstract :
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfonamide were examined as human β3 adrenergic receptor (AR) agonists. Notably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the β3 AR. Naphthyloxy compound 18 (β3 EC50=78 nM) did not activate the β1 and β2 ARs at 10 μM, and showed >1000-fold selectivity over binding to the β1 and β2 ARs.
