Molecular pharmacology

Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor

V Setola, M Dukat, RA Glennon, BL Roth

文献索引：Setola, Vincent; Dukat, Malgorzata; Glennon, Richard A.; Roth, Bryan L. Molecular Pharmacology, 2005 , vol. 68, # 1 p. 20 - 33

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被引用次数: 57

摘要

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 ...