SAR of psilocybin analogs: Discovery of a selective 5-HT2C agonist
Bioorganic & Medicinal Chemistry Letters August 3, 2005 Howard Sard, Govindaraj Kumaran, Cynthia Morency et al. 78 citations
A structure-activity relationship study of psilocybin and psilocin derivatives found that 1-methylpsilocin acts as a selective agonist at the human 5-HT(2C) receptor. Its phosphate derivative, 1-methylpsilocybin, and 4-fluoro-N,N-dimethyltryptamine each showed efficacy in an animal model of obsessive-compulsive disorder. These findings point to a new avenue for developing novel 5-HT(2C) receptor agonists with potential applications in drug discovery.