241467-58-3Relevant academic research and scientific papers
Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human β3 adrenergic receptor agonists
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)
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.
Fused piperidine substituted arylsulfonamides as beta 3-agonists
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, (2008/06/13)
Fused piperidine substituted arylsulfonamides are beta 3 adrenergic receptor agonists with very little beta 1 and beta 2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
