SAR of psilocybin analogs: Discovery of a selective 5-HT2C agonist
Howard Sard, Govindaraj Kumaran, Cynthia Morency, Bryan L. Roth, Beth Ann Toth, Ping He, Louis Shuster
Bioorganic & Medicinal Chemistry Letters August 3, 2005 DOI: 10.1016/j.bmcl.2005.06.104 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Structure-activity relationship study Peer reviewed |
|---|---|
| Interventions | 1-methylpsilocybin 4-fluoro-N N-dimethyltryptamine |
| Topics | Psilocybin Serotonin |
| Keywords | Agonist Pharmacology Hallucinogen Drug discovery Stereochemistry |
| Citations | 78 |
| Key points | 1-methylpsilocin is a selective agonist at the h5-HT(2C) receptor, and both 1-methylpsilocybin and 4-fluoro-N,N-dimethyltryptamine show efficacy in an animal model for obsessive-compulsive disorder. |
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.
Citations in the library
Cited by 49
- Psilocybin-Induced Decrease in Amygdala Reactivity Correlates with Enhanced Positive Mood in Healthy Volunteers Biological Psychiatry April 26, 2014
- The neural basis of psychedelic action. Nature Neuroscience October 24, 2022
- Psilocybin-Induced Deficits in Automatic and Controlled Inhibition are Attenuated by Ketanserin in Healthy Human Volunteers Neuropsychopharmacology September 28, 2011
- Differential contributions of serotonin receptors to the behavioral effects of indoleamine hallucinogens in mice Journal of Psychopharmacology December 8, 2010
- PSD-95 Is Essential for Hallucinogen and Atypical Antipsychotic Drug Actions at Serotonin Receptors Journal of Neuroscience June 3, 2009
and 44 more in the library
Cites 4
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