SAR of psilocybin analogs: discovery of a selective 5-HT 2C 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.
Sard
Howard
H
Organix Inc., 240 Salem Street, Woburn, MA 01801, USA. sard@organixinc.com
Kumaran
Govindaraj
G
Morency
Cynthia
C
Roth
Bryan L
BL
Toth
Beth Ann
BA
He
Ping
P
Shuster
Louis
L
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
D058826:Serotonin 5-HT2 Receptor Agonists; D017366:Serotonin Receptor Agonists; D011562:Psilocybin