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Metabolism of psilocybin and psilocin: clinical and forensic toxicological relevance

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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.

Dinis-Oliveira, R. J. (2016). METABOLISM OF PSILOCYBIN AND PSILOCIN: CLINICAL AND FORENSIC TOXICOLOGICAL RELEVANCE. Drug Metabolism Reviews, (just-accepted), 1-21. 10.1080/03602532.2016.1278228
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