Cited by 225Forensic Toxicology and Drug AnalysisPsychedelics and Drug StudiesPharmacogenetics and Drug Metabolism

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Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance

Dinis-Oliveira, Ricardo Jorge·2017·Drug Metabolism Reviews

DOI 10.1080/03602532.2016.1278228

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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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Kuypers, K. P. C., Mason, N. L., Carlier, A., Totomanova, I., & Haijen, E. C. H. M. (2026) · Molecular Psychiatry · doi:10.1038/s41380-026-03801-2 · Cited by 2
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“Cross-tolerance has been reported between LSD and other psychedelics such as psilocybin (Dinis-Oliveira, 2017).”
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Unveiling the Psychedelic Journey: An Appraisal of Psilocybin as a Profound Antidepressant Therapy
Shah, F. I., Shehzadi, S., Akram, F., Haq, I. U., Javed, B., Sabir, S., Kazim, Y., & Ashfaq, S. (2023) · Molecular Biotechnology · doi:10.1007/s12033-023-00994-7 · Cited by 4
“This underscores the pivotal role of psilocin as the primary active compound in the system [47].”
Investigating novel pharmacological strategies for treatment-resistant depression: focus on new mechanisms and approaches
de Miranda, A. S., Toscano, E. C. D. B., Venna, V. R., Graeff, F. G., & Teixeira, A. L. (2025) · Expert Opinion on Drug Discovery · doi:10.1080/17460441.2025.2460674 · Cited by 3
“Psilocybin and DMT are the most investigated in TRD. Psilocybin, a pro-drug of psilocin, is the psychoactive alkaloid of certain mushrooms [117].”
The psychedelic renaissance: psilocybin, a breakthrough for treatment resistant depression?
Norman, T. R. (2025) · Exploration of neuroscience · doi:10.37349/en.2025.1006105 · Cited by 2
Case Report: Resolution of Rheumatoid Arthritis in a Patient Consuming Psilocybin Mushrooms
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Production and extraction of psilocybin and psilocin from Psilocybe spp. mushrooms
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Self-citation
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“Many studies now connect the microbiome and receptors in the gut to the CNS through the gut-brain axis (GBA) 52 .”
Mild and Chemoselective Triethylsilane-Mediated Debenzylation for Phosphate Synthesis
Hodson, L. E., Tholath, P. J., Jacobs, L., Pribut, N., Pashikanti, G., van der Westhuyzen, A. E., Laws, D., & Liotta, D. C. (2024) · Organic Letters · doi:10.1021/acs.orglett.4c04258 · Cited by 1
Psilocin alleviates acute itch in mice: possible involvement of 5-HT2A receptors and kynurenine pathway
Afrooghe, A., Ahmadi, E., Lesani, A., Mehranjani, M. S., Elahi, M. M., Babaei, M., Shayan, M., Shafaroodi, H., Jafari, R. M., Foroumadi, A., et al. (2025) · Naunyn-Schmiedeberg s Archives of Pharmacology · doi:10.1007/s00210-025-04152-5 · Cited by 1
“Upon dephosphorylation, psilocybin converts to its bioactive metabolite, psilocin (Dinis-Oliveira 2017).”
Therapeutic Effects of Low-Dose Psilocybin in Depression and Other Mental Disorders: A Systematic Review
Meshkat, S., Fang, H., Sousa-Ho, R., Zeifman, R. J., Dunkley, B. T., Reichelt, A. C., Zhang, Y., Burback, L., Winkler, O., Greenshaw, A. J., et al. (2025) · Psychedelic Medicine · doi:10.1089/psymed.2024.0039 · Cited by 2
“5 Given its structural similarity to serotonin, psilocin functions as a partial agonist at 5-hydroxytryptamine (5-HT) receptors, particularly 5-HT 2A receptors.”
Clinical pharmacology
Vogt, S. B., & Liechti, M. E. (2025) · International review of neurobiology · doi:10.1016/bs.irn.2025.02.003 · Cited by 1
4‐HIAA Blocks Methamphetamine‐Induced Conditioned Place Preference in Mice Through Modulation of the 5‐HT Pathway in the Nucleus Accumbens
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Synthesis of Psilocin, Psilocybin and 5‐MeO‐DMT Succinate, All Labelled With Carbon‐14 at the Indole 2‐Position
Brown, R., Hamilton, N. M., Mallon, C., Stevenson, J., Faley, M. T., Kargbo, R. B., Sherwood, A. M., & Upeandran, B. (2025) · Journal of Labelled Compounds and Radiopharmaceuticals · doi:10.1002/jlcr.4155 · Cited by 1
Epigenome-wide association study of psilocybin-induced methylome changes in alcohol use disorder
Urban, M. M., Zillich, E., Rieser, N. M., Herdener, M., Spanagel, R., Vollenweider, F. X., Preller, K. H., & Meinhardt, M. W. (2026) · Translational Psychiatry · doi:10.1038/s41398-026-03961-3 · Cited by 1
“This selection comprised (i) receptors presumably involved in the effects of or targeted by psilocin, the active metabolite of psilocybin [50], namely HTR2A, HTR1A, SLC6A4, NTRK2, GRM2, DRD1 , and DRD2 [51 – 56]; (ii) immediate early genes (IEGs) and plasticity-related genes associated with…”
Psilocybin alleviates high-glucose and high-lipid-induced skin aging in BJ5Ta fibroblasts
Norouzkhani, F., Gojani, E. G., Wang, B., Li, D., Shujat, S., Shrestha, A., Rodriguez‐Juarez, R., Kovalchuk, O., & Kovalchuk, I. (2025) · Biochemistry and Cell Biology · doi:10.1139/bcb-2025-0250 · Cited by 2
Psilocybin and Chronic Pain: A New Perspective for Future Pain Therapists?
Natoli, S., Cuomo, A., Marchesini, M., Luongo, L., Bianco, G. L., Guardamagna, V. A., & Yamaguchi, S. (2025) · Medical Sciences · doi:10.3390/medsci13040277 · Cited by 1
“It is believed that the effects of psilocybin on the serotoninergic system are mediated by psilocin, the active metabolite of psilocybin [35], which displays high-affinity agonism for the 5-HT7, 5-HT1D, and 5-HT2A, B, and C receptors [36].”
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Sex-specific increased reactivity of the PVT and prolonged PVT→CeA circuit engagement following psilocin administration
Effinger, D. P., Hoffman, J. L., Quadir, S. G., Rollison, C. S., Toedt, D., Sanchez, M. E., High, M. W., Hodge, C. W., & Herman, M. A. (2026) · Nature Communications · doi:10.1038/s41467-026-71481-1 · Cited by 1
Psilocybin induces stereotyped movements and reduces defensive responding in planarians through 5-hydroxytryptamine mechanisms
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“As of 2025, approximately 140 species of Inocybe have been reported from China (Fan and Bau 2010, 2013, 2014a, 2014b, 2017, 2020; Fan et al. 2013, 2018; Bau and Fan 2018; Deng et al. 2021; Li et al. 2021b, 2022b; Chen et al. 2024; Gao et al. 2025; Zhu et al. 2025), and approximately 23 species of…”
P.0623 The clinical relevance of the pharmacokinetics of psilocybin
Andreiev, A., Bucuci, E., Chue, J., Els, C., & Chue, P. S. (2021) · European Neuropsychopharmacology · doi:10.1016/j.euroneuro.2021.10.588 · Cited by 1
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Brito-da-Costa, A. M., da Silva, D. D., Madureira-Carvalho, Á., & Dinis‐Oliveira, R. J. (2022) · Springer eBooks · doi:10.1007/978-3-030-92392-1_130 · Cited by 1
Self-citation
Activity of prefrontal cortex serotonin 2A receptor expressing neurons is necessary for the head-twitch response of mice to psychedelic drug DOI in a sex-dependent mannerPreprint
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“This is important since the psychedelic experience may be an essential element in the therapeutic effect of drugs like psilocin, the active metabolite of psilocybin [41].”
Background
Psilocybin Therapy for Depression and Anxiety in Parkinson's Disease: An Open-Label Pilot TrialPreprint
Bradley, E., Sakai, K., Fernandes‐Osterhold, G., Szigeti, B., Ludwig, C., Ostrem, J. L., Tanner, C. M., Bock, M., Llerena, K., Finley, P. R., et al. (2024) · SSRN Electronic Journal · doi:10.2139/ssrn.4871260 · Cited by 1
The admissibility of criminal profiling in courtroom
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Psylocybin and Psilocin as new tools to fight depression: an overview of the Pharmacodynamic and pharmacokinetic mechanisms
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Self-citation
P03-21 Magic mushrooms and psilocybin: pharmacokinetics, pharmacodynamics, and clinical applications
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Self-citation
Mushroom, Psilocybin
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Psychedelikagestützte Psychotherapie in der Behandlung depressiver Störungen
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“Durch das Enzym alkalische Phosphatase erfolgt die Umwandlung von Psilocybin zu Psilocin durch Abspaltung einer Phosphatgruppe [38, 39].”
Background
use of psilocybin in the treatment of psychiatric disorders – review
Woźniak, J., BOGACZ, R., Gaik, M., Ewa, U. R. A. M., MAGDA, I., Womperski, K., & OSUCH, M. (2023) · Journal of Education Health and Sport · doi:10.12775/jehs.2023.43.01.009
P05-02: Assessment of the CYP450 inhibitory activity of psilocybin, psilocin, LSD, 5-MeO-DMT and mescaline: An in vitro study
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Self-citation
Evidencias y perspectivas del potencial antidepresivo del “alcaloide mágico” psilocibina: una revisión narrativa
Toledo, M. M. V. (2023) · Cultura y Droga · doi:10.17151/culdr.2023.28.35.5
“La psilocina, a diferencia de la prodroga psilocibina, tiene la capacidad de atravesar la barrera hematoencefálica, de manera que es la que produce efectos a nivel del sistema nervioso central (Dinis-Oliveira, 2017; Stebelska, 2013).”
Background
Combining Machine Learning, Molecular Dynamics, and Free Energy Analysis for (5ht)-2a Receptor Modulator ClassificationPreprint
Barakat, K., Yu, X., Eid, Y., Jama, M., Pham, D., Ahmed, M., & Attar, M. (2024) · SSRN Electronic Journal · doi:10.2139/ssrn.4758294
From Venerable Cultural Practices to Modern Psychological Solutions: Enter Entheogens into Mainstream Medicine
Kerna, N. A., Pruitt, K. D., Carsrud, N. D. V., Kadivi, K., Ngwu, D. C., Holets, H. M., Flores, J. V., Nnake, I., Azi, C. I., Anderson, J., et al. (2024) · European Journal of Arts Humanities and Social Sciences · doi:10.59324/ejahss.2024.1(3).10
“Psilocybin and psilocin bind primarily to serotonin receptors in the brain, inducing a wide range of perceptual, cognitive, and emotional alterations (Dinis-Oliveira, 2017; Lowe et al., 2021).”
Background
Psychedelics in the Battle Against Itch: Unmasking the Antipruritic Potential of Psilocin Via 5-Ht2a Receptors and Kynurenine PathwayPreprint
Afrooghe, A., Ahmadi, E., Lesani, A., Mehranjani, M. S., Elahi, M. M., Babaei, M., Shayan, M., Shafaroodi, H., Jafari, R. M., Foroumadi, A., et al. (2024) · SSRN Electronic Journal · doi:10.2139/ssrn.4891179

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
DOI: 10.1080/03602532.2016.1278228
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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Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance

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