Frontiers in Psychiatry
November 17, 2017
Kristýna Štefková, Monika Židková, Rachel R. Horsley et al.
82 citations
Methylone, a synthetic cathinone analog of ecstasy, is marketed as relatively safe but has caused fatalities from hyperthermia, serotonin syndrome, and multi-organ failure. In adolescent male Wistar rats, methylone (5, 10, 20 mg/kg subcutaneously) dose-dependently increased locomotion, reduced time in the open field center at 20 mg/kg, and induced stereotyped circling; its metabolite nor-methylone showed similar behavioral potency. Both drugs peaked in serum and brain at 30 minutes, with a serum-to-brain ratio of 1:7.97. Methylone also caused hyperthermia, more pronounced in group-housed rats, and 40 mg/kg was lethal to some animals. The findings suggest methylone acts like MDMA or amphetamine but with higher toxicity, posing risks of serotonin syndrome, especially in crowded settings.
Frontiers in Psychiatry
January 10, 2018
Klára Šíchová, Nikola Pinterová, Monika Židková et al.
28 citations
Mephedrone (MEPH) and its primary metabolite nor-mephedrone (nor-MEPH) were detected in the serum, brain, lungs, and liver of male Wistar rats, with the highest levels found in lungs. Maximum concentrations occurred at 30 minutes, and nor-MEPH levels exceeded those of the parent drug at 2 and 4 hours. Both drugs increased locomotion and altered its spatial distribution in a dose-dependent, rapid, and short-lasting manner, without disrupting prepulse inhibition. Behavioral effects disappeared within 40 minutes, but MEPH-induced rectal temperature elevations persisted for 3 hours even in singly housed rats, suggesting a dissociation between behavioral and hyperthermic effects that may contribute to prolonged somatic toxicity.
Addiction Biology
May 7, 2020
Nikola Pinterová, Rachel R. Horsley, Hynek Danda et al.
13 citations
Naphyrone, a synthetic cathinone similar to pyrovalerone, potently blocks monoamine transporters and produces stimulant and entactogen-like effects. In male Wistar rats, a single subcutaneous dose of 1 mg/kg reached peak concentrations in blood and tissues within 30 minutes, with prolonged elevation in the brain relative to serum. A higher dose of 20 mg/kg caused modest increases in body temperature and lasting hyperactivity in an open field test, while transiently improving sensorimotor gating as measured by prepulse inhibition. No acute toxicity was observed. The drug crosses the blood-brain barrier rapidly and is eliminated slowly, with effects matching its pharmacokinetics. Harm-reduction guidance should follow that for other stimulants and cathinones.
Xenobiotica
July 12, 2016
Monika Židková, Igor Linhart, Marie Balı́ková et al.
6 citations
The drug 5,6-Methylenedioxy-2-aminoindane (MDAI), a serotoninergic aminoindane sold as a substitute for banned stimulants and entactogens, is metabolized in rats primarily through oxidative demethylenation followed by O-methylation and N-acetylation, producing five main metabolites found as glucuronides and sulphates. Most of the administered MDAI was excreted unchanged. Minor metabolites formed by hydroxylation include cis- and trans-1-hydroxy- and 4-hydroxy derivatives. Identification of most metabolites was confirmed with synthesized reference standards.
Journal of analytical toxicology
January 31, 2024
Miroslava Bursová, Tomáš Hložek, Miloš Sokol et al.
5 citations
A 42-year-old man who used drugs died at home and his body was found two months later. Autopsy did not reveal an obvious cause of death, but toxicology screening using liquid chromatography and mass spectrometry detected methoxetamine (MXE), a ketamine analog, and several of its metabolites in blood, urine, and gastric contents. MXE concentrations were 3.6 ng/mL in blood, 70.5 ng/mL in urine, and 18.0 ng/mL in gastric content. No other drugs or poisons were found, so despite the low blood level, MXE likely contributed to the death. The case shows that MXE and its metabolites can be detected in a decomposing body even after two months.