SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist

…, C Morency, BL Roth, BA Toth, P He, L Shuster

Index: Sard, Howard; Kumaran, Govindaraj; Morency, Cynthia; Roth, Bryan L.; Toth, Beth Ann; He, Ping; Shuster, Louis Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 20 p. 4555 - 4559

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Citation Number: 42

Abstract

An SAR study of psilocybin and psilocin derivatives reveals that 1-methylpsilocin is a selective agonist at the h5-HT2C receptor. The corresponding phosphate derivative, 1- methylpsilocybin, shows efficacy in an animal model for obsessive–compulsive disorder, as does 4-fluoro-N, N-dimethyltryptamine. These results suggest a new area for development of novel 5-HT2C agonists with applications for drug discovery.