Hynek Danda, Kristýna Mazochová, Klára Šíchová, Vladimír Mazoch, Lucie Olejníková-Ladislavová, Kateřina Syrová, Bronislav Jurásek, Petra Cihlářová, Radek Jurok, Tomáš Páleníček, Martin Kuchař
{"title":"Behavioural and pharmacological evaluation of the psilocybin analogue baeocystin in Wistar rats.","authors":"Hynek Danda, Kristýna Mazochová, Klára Šíchová, Vladimír Mazoch, Lucie Olejníková-Ladislavová, Kateřina Syrová, Bronislav Jurásek, Petra Cihlářová, Radek Jurok, Tomáš Páleníček, Martin Kuchař","doi":"10.1016/j.pnpbp.2025.111439","DOIUrl":null,"url":null,"abstract":"<p><p>Baeocystin is a naturally occurring tryptamine-based compound found in various psychoactive mushrooms, including in several species of Psilocybe genus. Due to its structural similarity to psilocybin, which has shown a therapeutic potential in treatment of psychiatric disorders, there is a growing interest in investigating whether baeocystin exhibits comparable effects. This study investigated the pharmacokinetic profile and acute behavioural effects of baeocystin in Wistar rats. Behavioural assessments including locomotor activity and its spatial characteristics (in the open field test) and sensorimotor gating measured by prepulse inhibition were evaluated after subcutaneous administration of 1.25 or 5 mg/kg baeocystin. Pharmacokinetics and brain-serum ratios were analysed after the 5 mg/kg sc. dose. Pharmacokinetics demonstrated that both baeocystin and its metabolite, norpsilocin, have a very limited ability to cross the blood-brain barrier. Consistent with the pharmacokinetic profile, baeocystin had no significant effects on locomotor activity, exploratory behaviour, anxiety-like responses, or sensorimotor gating at doses of either 1.25 or 5 mg/kg. In conclusion, our results suggest that baeocystin has minimal to no behavioural effects in rats, probably due to its poor permeability across the blood-brain barrier. This limited penetration may account for its negligible neurobiological and psychedelic activity.</p>","PeriodicalId":54549,"journal":{"name":"Progress in Neuro-Psychopharmacology & Biological Psychiatry","volume":" ","pages":"111439"},"PeriodicalIF":5.3000,"publicationDate":"2025-07-05","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in Neuro-Psychopharmacology & Biological Psychiatry","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1016/j.pnpbp.2025.111439","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CLINICAL NEUROLOGY","Score":null,"Total":0}
引用次数: 0
Abstract
Baeocystin is a naturally occurring tryptamine-based compound found in various psychoactive mushrooms, including in several species of Psilocybe genus. Due to its structural similarity to psilocybin, which has shown a therapeutic potential in treatment of psychiatric disorders, there is a growing interest in investigating whether baeocystin exhibits comparable effects. This study investigated the pharmacokinetic profile and acute behavioural effects of baeocystin in Wistar rats. Behavioural assessments including locomotor activity and its spatial characteristics (in the open field test) and sensorimotor gating measured by prepulse inhibition were evaluated after subcutaneous administration of 1.25 or 5 mg/kg baeocystin. Pharmacokinetics and brain-serum ratios were analysed after the 5 mg/kg sc. dose. Pharmacokinetics demonstrated that both baeocystin and its metabolite, norpsilocin, have a very limited ability to cross the blood-brain barrier. Consistent with the pharmacokinetic profile, baeocystin had no significant effects on locomotor activity, exploratory behaviour, anxiety-like responses, or sensorimotor gating at doses of either 1.25 or 5 mg/kg. In conclusion, our results suggest that baeocystin has minimal to no behavioural effects in rats, probably due to its poor permeability across the blood-brain barrier. This limited penetration may account for its negligible neurobiological and psychedelic activity.
期刊介绍:
Progress in Neuro-Psychopharmacology & Biological Psychiatry is an international and multidisciplinary journal which aims to ensure the rapid publication of authoritative reviews and research papers dealing with experimental and clinical aspects of neuro-psychopharmacology and biological psychiatry. Issues of the journal are regularly devoted wholly in or in part to a topical subject.
Progress in Neuro-Psychopharmacology & Biological Psychiatry does not publish work on the actions of biological extracts unless the pharmacological active molecular substrate and/or specific receptor binding properties of the extract compounds are elucidated.