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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Humans
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Mice
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Psilocybin / chemistry*
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Psilocybin / pharmacology*
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Serotonin 5-HT2 Receptor Agonists*
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Serotonin Receptor Agonists / chemistry*
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Serotonin Receptor Agonists / pharmacology*
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Structure-Activity Relationship
Substances
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Serotonin 5-HT2 Receptor Agonists
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Serotonin Receptor Agonists
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Psilocybin