Discovery of L-755,507: a subnanomolar human beta 3 adrenergic receptor agonist |
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| Authors: | ER Parmee HO Ok MR Candelore L Tota L Deng CD Strader MJ Wyvratt MH Fisher AE Weber |
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| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, Rahway, New Jersey 07065, USA. |
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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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