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.
Journal of ethnopharmacology
January 30, 2025
Maria Rita Garcia, Federico Ferreres, Tiago Mineiro et al.
3 citations
An aqueous extract of the aerial parts of Calea zacatechichi, a plant traditionally used for its dream-inducing effects, interferes with the cholinergic and dopaminergic systems by inhibiting acetylcholinesterase and tyrosinase, but does not affect monoamine oxidase A. The extract also shows notable cytotoxicity in neuronal and microglial cells at low concentrations, with evidence of apoptosis and necroptosis, though it scavenges free radicals and inhibits lipid peroxidation. Twenty-eight phenolic constituents were identified, 24 previously unreported in this species. The findings highlight the need for a regulatory framework for recreational use and help clarify the plant's psychopharmacological mechanisms.
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.