Drug Metabolism Reviews
January 2, 2017
Ricardo Jorge Dinis-Oliveira
221 citations
Psilocybin and psilocin, the main hallucinogenic compounds in magic mushrooms, act as agonists or partial agonists at 5-HT2A receptors. Psilocybin is a pro-drug dephosphorylated by alkaline phosphatase to the active metabolite psilocin, which is further metabolized; psilocin-O-glucuronide is the main urinary metabolite with clinical and forensic relevance. Considerable physiological variability between individuals influences dose-response and toxicological profiles. The review presents all major and minor psychoactive metabolites of psilocybin and psilocin.
Pharmaceuticals (Basel)
October 23, 2020
Andreia Machado Brito-Da-Costa, Diana Dias-Da-Silva, Nelson G. M. Gomes et al.
111 citations
Ayahuasca's psychoactive effects stem from the interplay of its alkaloids: N,N-dimethyltryptamine (DMT), harmine, harmaline, and tetrahydroharmine. DMT is rapidly absorbed and metabolized, but its oral activity requires monoamine oxidase inhibition by β-carbolines (harmine, harmaline) to prevent breakdown. Harmine and harmaline are quickly metabolized, while tetrahydroharmine has a longer half-life. The pharmacokinetics and pharmacodynamics of these compounds influence the duration and intensity of subjective effects, as well as potential toxicity. Understanding these processes is crucial for clinical management of adverse reactions and for forensic interpretation in cases of intoxication or death.
RevSALUS - Revista Científica da Rede Académica das Ciências da Saúde da Lusofonia
April 6, 2022
Joana Margarida Costa Fernandes, Cesar Filho, Andreia Machado Brito-da-Costa et al.
2 citations
No Summary
Science Letters
April 17, 2026
Francisco Sacadura, Cláudia Marques, Andreia Machado Brito-Da-Costa et al.
Both pure psilocybin and a Psilocybe cubensis extract altered the gut microbiota of male Wistar Han rats over two weeks. Fecal samples analyzed by 16S rRNA amplicon sequencing showed that microbial community structure shifted away from baseline and control profiles at day 7 and diverged further by day 14. The effect was more pronounced in rats given pure psilocybin than in those given the whole mushroom extract, suggesting the extract's additional compounds may modulate the impact. The results indicate a time-dependent modulation of gut microbiota by both treatments, with differential magnitude between the pure compound and the whole extract.
Science Letters
April 17, 2026
Beatriz P. Senra, Ricardo Jorge Dinis-Oliveira, Carlos J. A. Ribeiro
Psilocybe cubensis mushrooms contain psilocybin (0.5%–1.5% in dried mushrooms) and psilocin, which have therapeutic potential and are used recreationally. An optimized extraction method using cold methanol with 10% water and kinetic maceration yielded 1.98% psilocybin and 0.10% psilocin. A thin-layer chromatography (TLC) method with Ehrlich's reagent was developed for rapid identification of these tryptamines, suitable for forensic applications.
Science Letters
April 17, 2026
Diana Dias Da Silva, Andreia Machado Brito-Da-Costa, Francisco Sacadura et al.
Pure psilocybin and whole Psilocybe cubensis extract produce distinct behavioral and toxicological effects in male Wistar Han rats. Pure psilocybin decreased conditioned place preference scores at days 1 and 7, indicating aversive or non-reinforcing effects, and reduced exploratory activity. The extract did not significantly alter preference but transiently increased exploratory behavior at day 7. Peripherally, pure psilocybin increased relative liver weight, suggesting hepatic stress, while the extract reduced renal lipid peroxidation, indicating a protective or antioxidant effect likely from other compounds. These differences highlight the importance of matrix effects in psychedelic research.
Psychoactives
April 1, 2026
Ricardo Jorge Dinis-Oliveira
No Summary
RevSALUS - Revista Científica da Rede Académica das Ciências da Saúde da Lusofonia
January 1, 2025
Andreia Machado Brito Da Costa, Ricardo Jorge Dinis-Oliveira, Áurea Madureira-Carvalho et al.
Psychedelic compounds such as LSD, psilocin, psilocybin, 5-MeO-DMT, and mescaline show distinct neurotoxicity profiles in human neuroblastoma cells. LSD was the most cytotoxic, with EC50 values of 0.23 mM (MTT) and 0.57 mM (NR), while psilocin showed moderate toxicity (EC50 0.42 mM MTT, 0.69 mM NR). Psilocybin did not reach an EC50 within the tested range, indicating minimal toxicity. 5-MeO-DMT and mescaline affected cell viability only at higher concentrations (EC50 1.17–1.69 mM). Pre-treatment with any of these compounds did not significantly protect against glutamate-induced toxicity, suggesting limited neuroprotective potential in this model.
Pharmaceuticals (Basel, Switzerland)
February 25, 2021
Carolina Lobato-Freitas, Andreia Machado Brito-Da-Costa, Ricardo Jorge Dinis-Oliveira et al.
ADB-FUBINACA and AMB-FUBINACA are synthetic cannabinoids up to 140 and 85 times more potent than THC, the main psychoactive compound in cannabis. First synthesized in 2009, ADB-FUBINACA appeared recreationally in Japan in 2013, with fatal cases by 2015; AMB-FUBINACA emerged in 2014 and has caused multiple intoxication and death outbreaks. When smoked, effects begin within 10 to 15 seconds and last up to 60 minutes. Both act as full agonists at the CB1 receptor, producing cardiovascular and neurological effects such as altered perception, agitation, anxiety, paranoia, hallucinations, loss of consciousness, chest pain, hypertension, tachycardia, and seizures. The review calls for more research on their toxicokinetics to improve detection and treatment.