Archives of toxicology
August 1, 2015
Ana Margarida Araújo, Félix Carvalho, Maria de Lourdes Bastos et al.
290 citations
Tryptamines are a broad class of hallucinogens that act primarily as agonists of the 5-HT2A receptor, producing profound changes in sensory perception, mood, and thought. Historically, natural tryptamines like psilocybin and DMT have been used in ritual contexts, but synthetic tryptamines such as AMT, 5-MeO-DMT, and 5-MeO-DIPT have recently emerged as recreational drugs, often sold as 'research chemicals' online. Reports of intoxication and deaths have raised international concern, though the lack of pharmacological and toxicological data hampers assessment of their public health harm. This review covers historical background, prevalence, patterns of use, legal status, chemistry, toxicokinetics, toxicodynamics, and physiological and toxicological effects in animals and humans.
Toxicology
January 5, 2005
Helena Carmo, Jan G Hengstler, Douwe De Boer et al.
85 citations
The psychoactive designer drug 2C-B is broken down by liver cells from humans, monkeys, dogs, rabbits, rats, and mice through oxidative deamination and demethylation, producing several metabolites. A previously unknown metabolite, 4-bromo-2,5-dimethoxy-phenol (BDMP), appeared only in mouse cells, while another metabolite, 2-(4-bromo-2-hydroxy-5-methoxyphenyl)-ethanol (B-2-HMPE), formed in human, monkey, and rabbit cells but not in dog, rat, or mouse cells. Toxic effects on liver cells varied little across species but showed large differences among cells from three human donors, indicating that individual human variation may be more important than species differences in determining 2C-B toxicity.
Chemical Research in Toxicology
April 27, 2004
Márcia Carvalho, Fernando Remião, Nuno Milhazes et al.
77 citations
MDMA (ecstasy) and its major metabolite MDA did not directly damage heart cells from adult rats in the lab, but two further metabolites, N-Me-alpha-MeDA and alpha-MeDA, caused significant toxicity. These catechol metabolites triggered a loss of normal cell shape, depletion of the antioxidant glutathione, sustained increases in intracellular calcium, drops in ATP, and reduced activity of antioxidant enzymes. N-Me-alpha-MeDA was the most toxic. The findings suggest that MDMA must be metabolized into these catechol compounds for cardiotoxicity to occur in isolated heart cells.
JOURNAL OF HEALTH SCIENCE
January 1, 2007
Carla Macedo, Paula S. Branco, Luı́sa M. Ferreira et al.
36 citations
The neurotoxic effects of MDMA (Ecstasy) may depend heavily on how the body metabolizes the drug in the liver. Metabolism produces highly reactive compounds, including catechols, catechol thioethers, and quinones. Researchers used cyclic voltammetry to measure the electrochemical oxidation-reduction processes of chemically synthesized human MDMA metabolites. They then correlated the redox potentials of α-methyldopamine, N-methyl-α-methyldopamine, and 5-(glutathion-S-yl)-α-methyldopamine with their toxicity to rat cortical neurons. The data demonstrated that the lower oxidation potential of the catecholic thioether of α-MeDA correlated with its higher toxicity, supporting the use of voltammetry data to predict the toxicity of MDMA metabolites.
Journal of chromatography. B, Analytical technologies in the biomedical and life sciences
November 25, 2004
Helena Carmo, Douwe De Boer, Fernando Remião et al.
32 citations
The psychoactive drug 2C-B, sold as 'Ecstasy', is metabolized in mice, producing several metabolites detectable in urine by GC/MS. Unchanged 2C-B and these metabolites were identified, providing data that may help understand the drug's biological and toxicological effects and aid forensic analysis of samples from human abusers.
Forensic science international
September 1, 2014
Fernando Xavier Moreira, Félix Carvalho, Maria De Lourdes Bastos et al.
13 citations
Products containing the hallucinogenic plant Salvia divinorum, sold legally in smartshops and online, often mislead consumers about their potency and composition. Analysis of 10 such products, labeled with potencies from 5x to 60x, found that salvinorin A was the primary hallucinogen, along with three related compounds. Labeled concentrations of salvinorin A frequently did not match the actual amounts, and the true concentrations far exceeded the level needed to produce hallucinogenic effects. Safety information was often omitted, encouraging recreational use without adequate warnings.
PLoS ONE
June 14, 2016
João Martins, Miguel Castelo-Branco, Ana Batista et al.
10 citations
A single dose of MDMA (ecstasy) given to rats temporarily alters retinal function, as measured by electroretinograms. Three hours after administration, both MDMA-treated and high-temperature control rats showed larger and faster retinal responses, suggesting that the acute effects are partly due to MDMA-induced hyperthermia. After 24 hours, MDMA-treated animals still had increased responses in the outer retinal layers (photoreceptors and bipolar cells), even after temperature effects subsided, indicating a direct subacute effect of the drug. These changes returned to normal within seven days. The findings provide direct evidence that MDMA can enhance outer retinal activity, which may help explain visual disturbances reported by human users.
Elsevier eBooks
January 1, 2021
Daniela Călina, Félix Carvalho, Anca Oana Docea
9 citations
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