title: SAR of psilocybin analogs: discovery of a selective 5-HT 2C agonist.
abstract: 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.
authors.affiliation: Organix Inc., 240 Salem Street, Woburn, MA 01801, USA. sard@organixinc.com
authors.forename: Howard
authors.initials: H
authors.lastname: Sard
authors.forename: Govindaraj
authors.initials: G
authors.lastname: Kumaran
authors.forename: Cynthia
authors.initials: C
authors.lastname: Morency
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
authors.forename: Beth Ann
authors.initials: BA
authors.lastname: Toth
authors.forename: Ping
authors.initials: P
authors.lastname: He
authors.forename: Louis
authors.initials: L
authors.lastname: Shuster
mesh_terms: D000818:Animals; D006801:Humans; D051379:Mice; D011562:Psilocybin / Q000737:chemistry* / Q000494:pharmacology*; D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists / Q000737:chemistry* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists; D011562:Psilocybin