Bioorganic & Medicinal Chemistry Letters 1998-05-05

Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist.

E R Parmee, H O Ok, M R Candelore, L Tota, L Deng, C D Strader, M J Wyvratt, M H Fisher, A E Weber

Index: Bioorg. Med. Chem. Lett. 8(9) , 1107-12, (1998)

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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.

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