Archives of Toxicology
April 1, 2020
Dino Luethi, Matthias E. Liechti
258 citations
Designer drugs, which are chemically or pharmacologically similar to traditional drugs of abuse, continue to appear on the recreational market, often sold by internet vendors without legal restrictions. Their mechanisms of action and adverse effects generally mirror those of traditional drugs: stimulants like amphetamines and cathinones affect monoamine transporters and cause sympathomimetic effects; sedatives act on μ-opioid and GABA receptors, potentially leading to cardiorespiratory depression; dissociative drugs block NMDA receptors, similar to ketamine; synthetic cannabinoids target CB1 receptors, producing more severe adverse effects than cannabis; and serotonergic psychedelics act on 5-HT2A receptors to alter perception and...
Archives of Toxicology
July 5, 2020
Eline Pottie, Annelies Cannaert, Christophe P. Stove
36 citations
Serotonergic psychedelics, which act mainly through the serotonin 2A receptor, make up many new psychoactive substances. A stable cell-based bioassay using HEK 293 T cells was developed to monitor β-arrestin 2 recruitment to the 5-HT2AR. After verifying its performance against a transient transfection system, the assay was used to test 30 phenylalkylamine psychedelics: 12 phenethylamine derivatives (2C-X), 7 phenylisopropylamines (DOx), and 11 N-benzylderivatives (25X-NB). The resulting potency and efficacy values confirm findings from other in vitro assays and show a significant correlation with estimated common doses. This approach offers pharmacological insights and may help prioritize legal actions regarding the most potent compounds.
Archives of Toxicology
May 20, 2026
Caitlyn Norman, Dean Acreman, Meera Bissram et al.
Ethylbromazolam, a new designer benzodiazepine, has emerged in Canada, the UK, Australia, and Germany, with increasing detections since November 2024 and a concurrent decrease in bromazolam detections, likely due to bromazolam's international control on December 3, 2024. Other designer benzodiazepines like desalkylgidazepam and clobromazolam have also increased. In vitro patch clamp assays show ethylbromazolam has similar activity at the GABA-A receptor as bromazolam, with EC50 values of 10.1 nM and 15.2 nM respectively, indicating comparable pharmacological activity and potential harm. Ongoing market monitoring is recommended.
Archives of Toxicology
November 12, 2025
Gilles Salles, Carolina Aparecida de Faria Almeida, Isabella de Carvalho Alves et al.
Ayahuasca compounds N,N-dimethyltryptamine (DMT) and harmine (HRE), both alone and combined, partially protected human SH-SY5Y neuroblastoma cells from cocaine-induced toxicity. Cells exposed to cocaine with DMT and/or HRE showed increased viability compared to cocaine-only groups. Flow cytometry indicated partial to complete protection against apoptosis, and western blot revealed reduced expression of the apoptosis marker caspase-8 in co-treated cells. These findings suggest Ayahuasca-derived alkaloids merit further research for neuroprotection and treatment of substance use disorders.