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Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance
Abstract
Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the “magic mushrooms” and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic relevance but considerable physiological variability between individuals that can influence dose-response and toxicological profile has been reported. This review aims to discuss metabolism of psilocybin and psilocin, by presenting all major and minor psychoactive metabolites. Psilocybin is primarily a pro-drug that is dephosphorylated by alkaline phosphatase to active metabolite psilocin. This last is then further metabolized, psilocin-O-glucuronide being the main urinary metabolite with clinical and forensic relevance in diagnosis.
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“These findings may suggest an indirect role of the dopaminergic system in eliciting hallucinations, as interactions between serotonergic and dopaminergic systems have been established [33].”
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Background
Metadata
- Authors
- Dinis-Oliveira, R. J.
- Affiliations
- Department of Sciences, IINFACTS – Institute of Research and Advanced Training in Health Sciences and Technologies, University Institute of Health Sciences (IUCS), CESPU, CRL, Gandra, Portugal;
- Venue
- Drug Metabolism Reviews
- Publisher
- Informa UK Limited
- Published
- 2017-01-02
- Volume
- 49
- Issue
- 1
- Pages
- 84-91
- ISSN
- 0360-2532 (ISSN-L)
- 1097-9883
- OpenAlex
- W2572835720
- Cited by
- 224
- References
- 65
- Citations by year
- 2026: 21 · 2025: 48 · 2024: 41 · 2023: 38 · 2022: 36 · 2021: 10 · 2020: 17 · 2019: 7 · 2018: 6
- FWCI
- 1.17
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Drug Metabolism Reviews (publishedVersion)
- PubMed (publishedVersion)
- Funders
- Fundação para a Ciência e a Tecnologia
- FCT (IF/01147/2013)
- FEDER (UID/QUI/50006/2013)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Toxicology › Forensic Toxicology and Drug Analysis
- Social Sciences › Psychology › Clinical Psychology › Psychedelics and Drug Studies
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Keywords
- psilocybin, psilocin, drug metabolism, alkaline phosphatase, prodrugs, urinary metabolites, forensic toxicology, clinical toxicology, 5-HT2A receptor agonists, magic mushrooms, hallucinogens
- MeSH terms
- Hallucinogens, Humans, Prodrugs, Psilocybin, Metabolomics
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