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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“stimulating the release of dopamine in the caudate nucleus and putamen (Dinis-Oliveira 2017; Vollenweider, Vontobel, and Hell et al. 1999).”
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“The example of psilocybin and its metabolic product psilocin could be hilighted, which are two of the most studied hallucinogenic compounds from the psilocybin mushrooms [21].”
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“(3) where QT ci j is the change in QTc for subject i at time j; Intercept and Slope are the population mean intercept and population mean slope describing the relationship between psilocin concentration and QT c; ηI ntercept i and ηslopei are the random effects associated with the ith individual for the intercept and…”
BackgroundChemistry and Toxicology of Major Bioactive Substances in Inocybe Mushrooms
Patočka, J., Wu, R., Nepovimová, E., Vališ, M., Wu, W., & Kuča, K. (2021) · International Journal of Molecular Sciences · doi:10.3390/ijms22042218 · Cited by 46 · see citing works
“Psilocybin is primarily a pro-drug that is rapidly converted in the body through dephosphorylation by alkaline phosphatase to active metabolite psilocin [42].”
BackgroundRouaud, A., Calder, A. E., & Hasler, G. (2024) · Journal of Psychopharmacology · doi:10.1177/02698811231225609 · Cited by 44 · see citing works
“In contrast, based on the 15 nM affinity threshold, the risk of VHD would be substantial for both LSD and psilocybin: LSD has a Ki value of 0.98 nM at 5-HT2BR, and psilocybin’s active metabolite psilocin has a Ki of 4.6 nM at 5-HT2BR (Figure 1) (Dinis-Oliveira, 2017; McKenna and Peroutka, 1989).”
BackgroundInfluentialBrito-da-Costa, A. M., da Silva, D. D., Gomes, N. G. M., Dinis‐Oliveira, R. J., & Madureira-Carvalho, Á. (2021) · Pharmaceuticals · doi:10.3390/ph14020116 · Cited by 44 · see citing works
“Although not having affinity for the 5-HT2A receptors known to mediate the hallucinogenic properties of the classic psychedelics, such as lysergic acid diethylamide (LSD), psilocybin [12], mescaline [13], and N,N-dimethyltryptamine (DMT) [14], salvinorin A induces similar psychoactive effects, including perceptual dis…”
BackgroundSelf-citationPsilocybin history, action and reaction: A narrative clinical review
Sharma, P., Nguyen, Q. A., Matthews, S. J., Carpenter, E., Matthews, D. B., Patten, C. A., & Hammond, C. J. (2023) · Journal of Psychopharmacology · doi:10.1177/02698811231190858 · Cited by 38 · see citing works
“Drug class and pharmacokinetics Psilocybin (O-phosphoryl-4-hydroxy-N,N-DMT) and psilocin (4-hydroxy-N,N-DMT) are tryptophan indole-based alkaloids found in hallucinogenic mushrooms (Dinis-Oliveira, 2017).”
BackgroundNóbrega, L. D. M., & Dinis‐Oliveira, R. J. (2018) · Drug Metabolism Reviews · doi:10.1080/03602532.2018.1448867 · Cited by 37 · see citing works
Self-citationStrumila, R., Nobile, B., Korsakova, L., Lengvenytė, A., Olié, É., López‐Castromán, J., Guillaume, S., & Courtet, P. (2021) · Pharmaceuticals · doi:10.3390/ph14121213 · Cited by 37 · see citing works
“Therefore, psilocybin should be considered as a pro-drug, and psilocin should be considered as the active metabolite [46].”
BackgroundPepe, M., Hesami, M., de la Cerda, K. A., Perreault, M. L., Hsiang, T., & Jones, A. M. P. (2023) · Biotechnology Advances · doi:10.1016/j.biotechadv.2023.108247 · Cited by 36 · see citing works
Seeking the Psilocybiome: Psychedelics meet the microbiota-gut-brain axis
Kelly, J. R., Clarke, G. A., Harkin, A., Corr, S. C., Galvin, S. D., Pradeep, V., Cryan, J. F., O’Keane, V., & Dinan, T. G. (2022) · International Journal of Clinical and Health Psychology · doi:10.1016/j.ijchp.2022.100349 · Cited by 38 · see citing works
“After ingestion, psilocybin is rapidly dephosphorylated by alkaline phosphatases in the intestine and liver to the biologically active psilocin, which is then absorbed from the stomach and small intestine into circulation and can cross the blood brain barrier (BBB) (Dinis-Oliveira, 2017).”
BackgroundInfluentialPsilocybin’s effects on cognition and creativity: A scoping review
Bonnieux, J. N., VanderZwaag, B., Premji, Z., Garcia‐Romeu, A., & García-Barrera, M. A. (2023) · Journal of Psychopharmacology · doi:10.1177/02698811231179801 · Cited by 35 · see citing works
“Psilocin has no direct effect on dopaminergic systems and therefore lacks the reinforcement mechanisms necessary for dependence to occur (Bienemann et al., 2020; Dinis-Oliveira, 2017; Nichols, 2016).”
BackgroundHonyiglo, E., Franchi, A., Cartiser, N., Bottinelli, C., Advenier, A., Bévalot, F., & Fanton, L. (2019) · Journal of Forensic Sciences · doi:10.1111/1556-4029.13982 · Cited by 35 · see citing works
“rooms contain other active substances like baeocystin or phenylethylamine, a sympathomimetic amine which can lead to cardiovascular disorders (2).”
BackgroundChadeayne, A. R., Pham, D. N. K., Reid, B. G., Golen, J. A., & Manke, D. R. (2020) · ACS Omega · doi:10.1021/acsomega.0c02208 · Cited by 35 · see citing works
Mushroom-derived nutraceuticals in the 21st century: an appraisal and future perspectives
Mayirnao, H.-S., Sharma, K., Jangir, P., Kaur, S., & Kapoor, R. (2024) · Journal of Future Foods · doi:10.1016/j.jfutfo.2024.07.013 · Cited by 33 · see citing works
Adverse pharmacokinetic interactions between illicit substances and clinical drugs
Abbott, K. L., Flannery, P. C., Gill, K. S., Boothe, D. M., Dhanasekaran, M., Mani, S., & Pondugula, S. R. (2019) · Drug Metabolism Reviews · doi:10.1080/03602532.2019.1697283 · Cited by 33 · see citing works
An Improved, Practical, and Scalable Five-Step Synthesis of Psilocybin
Kargbo, R. B., Sherwood, A. M., Meisenheimer, P. L., & Tarpley, G. (2020) · Synthesis · doi:10.1055/s-0039-1691565 · Cited by 33 · see citing works
Roberts, C. A., Osborne-Miller, I., Cole, J. C., Gage, S. H., & Christiansen, P. (2020) · Journal of Psychopharmacology · doi:10.1177/0269881120936508 · Cited by 32 · see citing works
“…(4-phosphoryloxy-N,N-dimethyltryptamine), along with its non-phosphorylated counterpart psilocin, is the primary psychoactive compound found within ‘magic’ mushrooms (Studerus et al., 2011), typically occurring at concentrations of 0.5–1% (m/m) per mushroom (Dinis-Oliveira, 2017; Freye, 2009).”
BackgroundInfluentialPsilocybin therapy for mood dysfunction in Parkinson’s disease: an open-label pilot trial
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. (2025) · Neuropsychopharmacology · doi:10.1038/s41386-025-02097-0 · Cited by 31 · see citing works
“While the toxicity of psilocybin is relatively low [15, 16], its safety for people with PD warrants careful evaluation.”
Coppola, M., Bevione, F., & Mondola, R. (2021) · Journal of Xenobiotics · doi:10.3390/jox12010004 · Cited by 25 · see citing works
The evolution and ecology of psilocybin in nature
Meyer, M. J., & Slot, J. C. (2023) · Fungal Genetics and Biology · doi:10.1016/j.fgb.2023.103812 · Cited by 30 · see citing works
Hernández-León, A., Escamilla-Orozco, R. I., Tabal-Robles, A. R., Martı́nez-Vargas, D., Romero-Bautista, L., Escamilla-Soto, G., Romero, O. S. G., Torres-Valencia, J. M., & González-Trujano, M. E. (2023) · Journal of Ethnopharmacology · doi:10.1016/j.jep.2023.117415 · Cited by 33 · see citing works
Pharmacokinetics of Psilocybin: A Systematic Review
Meshkat, S., Al-Shamali, H. F., Perivolaris, A., Tullu, T., Zeifman, R. J., Zhang, Y., Burback, L., Winkler, O., Greenshaw, A. J., Husain, M. I., et al. (2025) · Pharmaceutics · doi:10.3390/pharmaceutics17040411 · Cited by 29 · see citing works
“Psilocybin is a prodrug that undergoes rapid metabolism in the body to its active form, psilocin (N,N-dimethyl-4-hydroxytryptamine), mostly through gut and hepatic dephosphorylation [12].”
Beating pain with psychedelics: Matter over mind?
Elman, I., Pustilnik, A. C., & Borsook, D. (2021) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2021.12.005 · Cited by 28 · see citing works
Potential Therapeutic Effects of Psilocybin: A Systematic Review
Goel, D. B., & Zilate, S. (2022) · Cureus · doi:10.7759/cureus.30214 · Cited by 30 · see citing works
“2 mg/kg oral psilocybin showed a nonsignificant difference, compared to niacin [16,17].”
BackgroundResultPsilocybin as a Treatment for Psychiatric Illness: A Meta-Analysis
Irizarry, R., Winczura, A., Dimassi, O., Dhillon, N., Minhas, A., & Larice, J. (2022) · Cureus · doi:10.7759/cureus.31796 · Cited by 26 · see citing works
“Psilocin is usually detectable in the plasma within 20-40 minutes [7,8].”
BackgroundTamama, K., & Lynch, M. J. (2019) · Handbook of experimental pharmacology · doi:10.1007/164_2019_260 · Cited by 27 · see citing works
Pharmacological and behavioural effects of tryptamines present in psilocybin‐containing mushrooms
Rakoczy, R. J., Runge, G. N., Sen, A. K., Sandoval, O., Wells, H. G., Nguyen, Q., Roberts, B., Sciortino, J. H., Gibbons, W. J., Friedberg, L. M., et al. (2024) · British Journal of Pharmacology · doi:10.1111/bph.16466 · Cited by 25 · see citing works
“Quickly after ingesting “ magic ” mushrooms, for example psilocybin is enzymatically dephosphorylated by alkaline phosphatase, converting the compound from its prodrug form to its more active form, psilocin (Dinis-Oliveira, 2017; Horita, 1963; Horita & Weber, 1961a, 1961b).”
Wiens, K. R., Brooks, N. A. H., Riar, I., Greuel, B. K., Lindhout, I. A., & Klegeris, A. (2024) · Molecules · doi:10.3390/molecules29215084 · Cited by 25 · see citing works
“When ingested, psilocybin undergoes rapid dephosphorylation by alkaline phosphatase in the small intestine, kidneys, and plasma to yield psilocin, which freely crosses the blood–brain barrier and exerts psychotropic activity [27].”
BackgroundThe phosphate ester group in secondary metabolites.
Della-Felice, F., Bartolomeu, A. D. A., & Pilli, R. (2022) · Natural product reports (Print) · doi:10.1039/d1np00078k · Cited by 11 · see citing works
Wang, J., Liang, M., Shang, Q., Qian, H., An, R., Liu, H., Shao, G., Li, T., & Liu, X. (2023) · CNS Neuroscience & Therapeutics · doi:10.1111/cns.14054 · Cited by 24 · see citing works
“001), and significant main effects of time (F(1,20) = 4.”
BackgroundPsychedelic therapy in depression and substance use disorders
Korkmaz, N. D., Çıkrıkçılı, U., Akan, M., & Yücesan, E. (2024) · European Journal of Neuroscience · doi:10.1111/ejn.16421 · Cited by 25 · see citing works
“When metabolized in the bloodstream by alkaline phosphatases, it is converted to its active form, psilocin (Dinis-Oliveira, 2017).”
Do the therapeutic effects of psilocybin involve actions in the gut?
Reed, F. M., & Foldi, C. J. (2024) · Trends in Pharmacological Sciences · doi:10.1016/j.tips.2023.12.007 · Cited by 24 · see citing works
Meade, E., Hehir, S., Rowan, N. J., & Garvey, M. (2022) · Journal of Fungi · doi:10.3390/jof8030290 · Cited by 24 · see citing works
“A. muscaria contains many biologically active compounds including the psychoactive alkaloids: muscarine, ibotenic acid and muscimol [109] where ibotenic and muscimol are structurally similar to gamma-aminobutyric acid (GABA) having effect on glutamate receptors in the CNS [110] and can cross the BBB. Ibotenic acid is…”
BackgroundInfluentialPsilocybin, an Effective Treatment for Major Depressive Disorder in Adults - A Systematic Review
Watford, T., & Masood, N. (2024) · Clinical Psychopharmacology and Neuroscience · doi:10.9758/cpn.23.1120 · Cited by 23 · see citing works
“As a substituted indolealkylamine it is based upon the structure of tryptamine, illustrated in Figure 2, which acts as a predominant agonist in the serotonergic system at 5-hydroxytryptamine (5-HT) 1a and 2a/c subtype receptors [7].”
Dinis-Oliveira, R. J., & Magalhães, T. (2020) · Journal of Clinical Medicine · doi:10.3390/jcm9030770 · Cited by 23 · see citing works
“Hallucinogens, such as the diethylamide of lysergic acid (LSD), mescaline, psilocybin, and psilocin, also have a pronounced effect on workplace performance [52,53].”
BackgroundSelf-citationRaithatha, S. A., Hagel, J. M., Matinkhoo, K., Yu, L. X., Press, D., Cook, S. G., Sharma, G., Dhananjaya, D., Jensen, G., Lee, J. B., et al. (2023) · Journal of Medicinal Chemistry · doi:10.1021/acs.jmedchem.3c01225 · Cited by 22 · see citing works
Abuse of Magic Mushroom, Peyote Cactus, LSD, Khat, and Volatiles
Dasgupta, A. (2019) · Elsevier eBooks · doi:10.1016/b978-0-12-815607-0.00033-2 · Cited by 22 · see citing works
Otto, M. E., van der Heijden, K. V., Schoones, J. W., van Esdonk, M. J., Borghans, L. G. J. M., Jacobs, G. E., & van Hasselt, J. G. C. (2025) · Clinical Pharmacokinetics · doi:10.1007/s40262-024-01454-4 · Cited by 21 · see citing works
“In summary, metabolism occurs by dephosphorylation in the stomach by alkaline phosphatases or other non-specific esterases in the intestine and kidneys [11–14].”
Psychedelics and Psychedelic-Assisted Psychotherapy
Reiff, C. M., Richman, E. E., Nemeroff, C. B., Carpenter, L. L., Widge, A. S., Rodríguez, C. I., Kalin, N. H., & McDonald, W. M. (2021) · FOCUS The Journal of Lifelong Learning in Psychiatry · doi:10.1176/appi.focus.19104 · Cited by 21 · see citing works
Haniff, Z. R., Bocharova, M., Mantingh, T., Rucker, J., Velayudhan, L., Taylor, D. M., Young, A. H., Aarsland, D., Vernon, A. C., & Thuret, S. (2024) · Pharmacology & Therapeutics · doi:10.1016/j.pharmthera.2024.108641 · Cited by 21 · see citing works
“There is, however, evidence that it may bind other 5-HT receptor subtypes, receptor classes and monoamine transporters to a lesser extent (Blough et al., 2014; Dinis-Oliveira, 2017; Erkizia-Santamaría, Alles-Pascual, Horrillo, Meana, & Ortega, 2022a; Halberstadt & Geyer, 2011).”
Chadeayne, A. R., Golen, J. A., & Manke, D. R. (2019) · Acta Crystallographica Section E Crystallographic Communications · doi:10.1107/s2056989019007370 · Cited by 21 · see citing works
“When consumed orally, psilocybin hydrolyzes to generate psilocin, a serotonin-2a agonist, producing mood-altering or ‘psychedelic’ effects (Dinis-Oliveira, 2017).”
BackgroundJensen, M. E., Stenbæk, D. S., Messell, C., Poulsen, E. D., Varga, T. V., Fisher, P. M., Nielsen, M. K. K., Johansen, S. S., Volkow, N. D., Knudsen, G. M., et al. (2025) · Journal of Psychopharmacology · doi:10.1177/02698811251319457 · Cited by 21 · see citing works
“Future studies should also consider other important factors that may alter the metabolic pathway of psilocin, including the enzymes aldehyde dehydrogenase and uridine diphosphate (UDP)- glucuronosyltransferases (Dinis-Oliveira, 2017) which may be affected by chronic alcohol intake.”
Chronic Treatment With Psilocybin Decreases Changes in Body Weight in a Rodent Model of Obesity
Huang, J. Y., Pham, M. M., Panenka, W. J., Honer, W. G., & Barr, A. M. (2022) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2022.891512 · Cited by 20 · see citing works
Menéndez-Quintanal, L. M., Matey, J. M., González, V. D. F., Serrano, B. B., Hernández-Díaz, F. J., Zapata, F., Montalvo, G., & García‐Ruiz, C. (2024) · Psychoactives · doi:10.3390/psychoactives3040033 · Cited by 21 · see citing works
Polo-Castellano, C., Álvarez, J. Á., Palma, M., Barbero, G. F., Ayuso, J., & Ferreiro-González, M. (2022) · Journal of Fungi · doi:10.3390/jof8060598 · Cited by 20 · see citing works
“Its active form, psilocin (4-hydroxy-N,N-dimethyltryptamine) is a serotoninergic agonist [15] that binds to (5-HT)2A receptors causing the above-mentioned effects [16].”
BackgroundCardiovascular effects and safety of classic psychedelics
Nahlawi, A., Ptaszek, L. M., & Ruskin, J. N. (2025) · Nature Cardiovascular Research · doi:10.1038/s44161-025-00608-2 · Cited by 21 · see citing works
“56); and the distinct metabolic profile of each compound 57,58 .”
Molecular and Medical Aspects of Psychedelics
Wojtas, A., & Gołembiowska, K. (2023) · International Journal of Molecular Sciences · doi:10.3390/ijms25010241 · Cited by 21 · see citing works
Efficacy and safety of psilocybin for the treatment of substance use disorders: A systematic review
Meshkat, S., Malik, G., Zeifman, R. J., Swainson, J., Balachandra, K., Reichelt, A. C., Zhang, Y., Burback, L., Winkler, O., Greenshaw, A. J., et al. (2025) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2025.106163 · Cited by 21 · see citing works
Interpol review of controlled substances 2016–2019
Jones, N. S., & Comparin, J. H. (2020) · Forensic Science International Synergy · doi:10.1016/j.fsisyn.2020.01.019 · Cited by 18 · see citing works
“[786]; review [787]; characterization of four psilocybin biosynthesis enzymes [788]; 1D and 2D NMR spectroscopy and high-”
BackgroundDeciphering psilocybin: Cytotoxicity, anti-inflammatory effects, and mechanistic insights
Laabi, S., LeMmon, C., Vogel, C., Chacon, M., & Jimenez, V. M. (2024) · International Immunopharmacology · doi:10.1016/j.intimp.2024.111753 · Cited by 18 · see citing works
Immunochemical monitoring of psilocybin and psilocin to identify hallucinogenic mushrooms
Morita, I., Oyama, H., Kiguchi, Y., Oguri, A., Fujimoto, N., Takeuchi, A., Tanaka, R., Ogata, J., Kikura‐Hanajiri, R., & Kobayashi, N. (2020) · Journal of Pharmaceutical and Biomedical Analysis · doi:10.1016/j.jpba.2020.113485 · Cited by 17 · see citing works
Patra, A., & Mukherjee, A. K. (2022) · Toxicon · doi:10.1016/j.toxicon.2022.07.014 · Cited by 17 · see citing works
Psilocybin as a novel treatment for chronic pain
Askey, T., Lasrado, R., Maiarù, M., & Stephens, G. J. (2024) · British Journal of Pharmacology · doi:10.1111/bph.17420 · Cited by 17 · see citing works
“The elimination half-life of psilocin is approximately 50 min, with psychoactive effects typically lasting 4 – 6 h, depending on the dose and metabolism (Dinis-Oliveira, 2017).”
Vorobyeva, N. S., & Kozlova, A. A. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.927984 · Cited by 19 · see citing works
“These metabolites are excreted by the liver and kidney, however, enzymes involved in these reactions are unknown (Brown et al., 2017; Dinis-Oliveira, 2017).”
BackgroundXue, C., Li, J., Yu, L. X., Maule, F., Chang, L., Gallant, J. A., Press, D. J., Raithatha, S. A., Hagel, J. M., & Facchini, P. J. (2023) · Journal of Biological Chemistry · doi:10.1016/j.jbc.2023.105231 · Cited by 16 · see citing works
Psilocybin for clinical indications: A scoping review
Madden, K., Flood, B., Shing, D. Y., Ade‐Conde, A. M., Kashir, I., Mark, M., MacKillop, J. M., Bhandari, M., & Adili, A. F. (2024) · Journal of Psychopharmacology · doi:10.1177/02698811241269751 · Cited by 16 · see citing works
“These effects encompass changes in neurotransmitter release, notably dopamine and glutamate, and can modulate perception, emotions, thoughts, and symptoms of anxiety or elation (Dinis-Oliveira, 2017; López-Giménez and González-Maeso, 2018).”
BackgroundPsilocybin: From Psychiatric Pariah to Perceived Panacea
Fonzo, G. A., Wolfgang, A. S., Barksdale, B. R., Krystal, J. H., Carpenter, L. L., Kraguljac, N. V., Grzenda, A. L., McDonald, W. M., Widge, A. S., Rodríguez, C. I., et al. (2025) · American Journal of Psychiatry · doi:10.1176/appi.ajp.20230682 · Cited by 16 · see citing works
Study of the in vitro and in vivo metabolism of 4-HO-MET
Bruni, P. S., Grafinger, K. E., Nussbaumer, S., König, S., Schürch, S., & Weinmann, W. (2018) · Forensic Science International · doi:10.1016/j.forsciint.2018.06.037 · Cited by 15 · see citing works
Mushrooms as Promising Therapeutic Resources: Review and Future Perspectives
Badalyan, S. М., Morel, S., Barkhudaryan, A., & Rapior, S. (2023) · Springer eBooks · doi:10.1007/978-981-19-9550-7_1 · Cited by 15 · see citing works
Psychedelic Therapy: A Primer for Primary Care Clinicians—Psilocybin
Tabaac, B. J., Shinozuka, K., Arenas, A., Beutler, B. D., Cherian, K. N., Evans, V. D., Fasano, C., & Muir, O. S. (2024) · American Journal of Therapeutics · doi:10.1097/mjt.0000000000001724 · Cited by 16 · see citing works
“7 The half-life of psilocin is 108 minutes.”
BackgroundKinderlehrer, D. A. (2025) · Neuropsychiatric Disease and Treatment · doi:10.2147/ndt.s500337 · Cited by 15 · see citing works
Strauss, D., Ghosh, S. B., Murray, Z., & Gryzenhout, M. (2022) · 3 Biotech · doi:10.1007/s13205-022-03355-4 · Cited by 13 · see citing works
“However, both psilocybin and psilocin have been found to be soluble in methanol and ethanol (Dinis-Oliveira 2017).”
BackgroundA Review of Synthetic Access to Therapeutic Compounds Extracted from Psilocybe
Serreau, R., Amirouche, A., Benyamina, A., & Berteina‐Raboin, S. (2022) · Pharmaceuticals · doi:10.3390/ph16010040 · Cited by 13 · see citing works
Utility of preclinical models in the study of psilocybin – A comprehensive review
Pedicini, M., & Cordner, Z. A. (2023) · Neuroscience & Biobehavioral Reviews · doi:10.1016/j.neubiorev.2023.105046 · Cited by 13 · see citing works
Present and future of metabolic and metabolomics studies focused on classical psychedelics in humans
Madrid-Gambín, F., Fabregat‐Safont, D., Gomez‐Gómez, À., Olesti, E., Mason, N. L., Ramaekers, J. G., & Pozo, Ó. J. (2023) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2023.115775 · Cited by 14 · see citing works
“After consumption, psilocybin is rapidly metabolized to psilocin (4-OH-DMT) by intestinal alkaline phosphates and undetermined esterases [134], as illustrated in Fig.”
Harnessing Pharmacogenomics in Clinical Research on Psychedelic‐Assisted Therapy
Halman, A., Conyers, R. K., Moore, C., Khatri, D., Sarris, J. J., & Perkins, D. (2024) · Clinical Pharmacology & Therapeutics · doi:10.1002/cpt.3459 · Cited by 13 · see citing works
“43 In fact, MAO inhibitors (MAOIs) are also consumed with psilocybin to intensify its effects 42 and hy-pothetically, CYP2D6 activity could influence the effects of this combination.”
InfluentialMeccia, J., Lopez, J., & Bagot, R. C. (2022) · Psychopharmacology · doi:10.1007/s00213-022-06297-0 · Cited by 13 · see citing works
“Psilocin crosses the blood–brain barrier and directly binds with 5-HT receptors (5-HTRs) (Dinis-Oliveira 2017).”
BackgroundManagement of overdoses of salvia, kratom, and psilocybin mushrooms: a literature review
Reinert, J. P., Colunga, K. N., Etuk, A., Richardson, V., & Dunn, R. L. (2020) · Expert Review of Clinical Pharmacology · doi:10.1080/17512433.2020.1794811 · Cited by 13 · see citing works
“The psychoactive effects of psilocin usually subside within about four to six hours after it is excreted from the body [51].”
BackgroundExploring Psilocybe spp. mycelium and fruiting body chemistry for potential therapeutic compounds
Waldbillig, A., Baranova, M., Neumann, S., Andrade, J., & Sidhu, S. (2023) · Frontiers in Fungal Biology · doi:10.3389/ffunb.2023.1295223 · Cited by 13 · see citing works
“On oral administration in humans, psilocybin is rapidly converted to psilocin via intestinal alkaline phosphatase, where nearly 100% of the bioactive molecule is found in circulation 30 min to 6 h after ingestion (Dinis-Oliveira, 2017).”
BackgroundSakai, K., Bradley, E., Zamaria, J. A., Agin-Liebes, G., Kelley, D. P., Fish, A., Martini, V., Ferris, M. C., Morton, E. E., Michalak, E. E., et al. (2024) · Psychopharmacology · doi:10.1007/s00213-024-06585-x · Cited by 13 · see citing works
“Sixth, it is possible that there are meaningful differences between the synthetic psilo-cybin used in research settings and the psilocybin mush-rooms accessible in the community–few data are available regarding other psychoactive compounds found in mush-rooms (Dinis-Oliveira 2017).”
The fumarate salts of the N-isopropyl-N-methyl derivatives of DMT and psilocin
Chadeayne, A. R., Pham, D. N. K., Golen, J. A., & Manke, D. R. (2019) · Acta Crystallographica Section E Crystallographic Communications · doi:10.1107/s2056989019011253 · Cited by 12 · see citing works
“Upon digestion, psilocybin hydrolyses to generate psilocin, the 4-hydroxy derivative of DMT. Psilocin is a potent seratonin 2a-agonist, which is responsible for its psychoactive properties (Dinis-Oliveira, 2017; Nichols, 2012).”
BackgroundNeuroprotective effects of psilocybin in a rat model of stroke
Yu, S., Wu, K., Wang, Y.-S., Bae, E., Chianelli, F., Bambakidis, N. C., & Wang, Y. (2024) · BMC Neuroscience · doi:10.1186/s12868-024-00903-x · Cited by 10 · see citing works
“Psilocybin is dephosphorylated to the active metabolite psilocin by systemic alkaline phosphatase after peripheral administration [11, 38].”
BackgroundMedicinal Mushroom of Potential Pharmaceutical Toxic Importance: Contribution in Phytotherapy
Fokunang, E. T., Annih, M. G., Abongwa, L. E., Bi, M. E., Mayoudom, V. E. T., Fonmboh, D. J., & Fokunang, C. (2022) · IntechOpen eBooks · doi:10.5772/intechopen.103845 · Cited by 10 · see citing works
Polo-Castellano, C., Mateos, R. M., Visiedo, F., Palma, M., Barbero, G. F., & Ferreiro‐González, M. (2023) · Antioxidants · doi:10.3390/antiox12020369 · Cited by 10 · see citing works
“Many NPs present structural similarities with certain endogenous compounds [2].”
BackgroundRahbarnia, A., Li, Z., & Fletcher, P. J. (2023) · Psychopharmacology · doi:10.1007/s00213-023-06474-9 · Cited by 10 · see citing works
“Pharmacologically, psilocybin activates serotonin (5-HT) 2A receptors via its active metabolite psilocin (Dinis-Oliveira 2017).”
Jones, N., Wagner, L., Pellitteri-Hahn, M. C., Scarlett, C. O., & Wenthur, C. J. (2024) · Frontiers in Psychiatry · doi:10.3389/fpsyt.2023.1303365 · Cited by 10 · see citing works
- 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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