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Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist
E R Parmee1, H O Ok, M R Candelore
1Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
A study of 4-acylaminobenzenesulfonamides in a cloned human beta 3 adrenergic receptor assay resulted in the discovery of n-hexylurea, L-755,507 (22). This 0.43 nM beta 3 agonist, which is > 440-fold selective over both beta 1 and beta 2 binding, is among the most potent human beta 3 agonists reported to date.