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SAR of psilocybin analogs: discovery of a selective 5-HT2C agonist.

An SAR study of psilocybin and psilocin derivatives reveals that 1-methylpsilocin is a selective agonist at the h5-HT(2C) 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-HT(2C) agonists with applications for drug discovery.

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Journal: Bioorganic & Medicinal Chemistry Letters
Date: 2005-09-30
Source: Europe PMC
DOI: 10.1016/j.bmcl.2005.06.104
PubMed: 16061378

Authors

Sard H Kumaran G Morency C Roth BL Toth BA He P Shuster L.

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Topics and keywords

psilocybin psilocin OCD Receptor Pharmacology Animal Study Animal Study Animals Humans Mice Structure-Activity Relationship Serotonin Receptor Agonists Serotonin 5-HT2 Receptor Agonists Psilocybin

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SAR of psilocybin analogs: discovery of a selective 5-HT2C agonist.2005-09-30