Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human β3 adrenergic receptor agonists
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. (C) 2000 Elsevier Science Ltd.
Parmee, Emma R.,Brockunier, Linda L.,He, Jiafang,Singh, Suresh B.,Candelore, Mari R.,Cascieri, Margaret A.,Deng, Liping,Liu, Yong,Tota, Laurie,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
p. 2283 - 2286
(2007/10/03)
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