Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor
V Setola, M Dukat, RA Glennon, BL Roth
Index: Setola, Vincent; Dukat, Malgorzata; Glennon, Richard A.; Roth, Bryan L. Molecular Pharmacology, 2005 , vol. 68, # 1 p. 20 - 33
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Citation Number: 57
Abstract
Abstract S-(+)-Norfenfluramine (SNF)—an active metabolite of the now-banned anorexigen fenfluramine—has been implicated in the drug's appetite-suppressing actions and its life- threatening cardiovascular side effects. SNF reduces appetite through serotonin 5-HT 2C receptor activation; it causes cardiopulmonary side effects through 5-HT 2B receptor activation. Thus, we attempted to identify molecular determinants of SNF binding to 5-HT ...
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