Brain Research Bulletin
May 4, 2016
Rachel R. Horsley, Eva Lhotková, Kateřina Hájková et al.
38 citations
Methoxetamine (MXE), a novel psychoactive compound used as a substitute for ketamine, was tested in Wistar rats across a series of behavioral tasks. At lower doses (5 and 10 mg/kg), MXE stimulated locomotion, increased thigmotaxis, and decreased time spent in the center of an open field, indicating anxiogenic effects. At a higher dose (40 mg/kg), it reduced locomotion and increased time in the center, suggesting sedation or anesthesia. MXE disrupted prepulse inhibition (PPI) and reduced habituation. The drug accumulated in the brain, with brain-to-serum ratios between 2.06 and 2.93, and its effects lasted at least 60–90 minutes.
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.
Frontiers in Psychiatry
April 24, 2018
Rachel R. Horsley, Eva Lhotková, Kateřina Hájková et al.
20 citations
MDPV, a potent synthetic cathinone, is rapidly absorbed after subcutaneous injection in male Wistar rats, reaching peak concentrations in serum, brain, and lungs within 30 minutes. It readily crosses the blood-brain barrier, with a brain-to-serum ratio of about 2 lasting for roughly 120 minutes. The drug is primarily excreted as metabolites, with demethylenyl-MDPV and demethylenyl-methyl-MDPV levels three to four times higher than the parent drug in urine. MDPV acts as a typical stimulant, producing locomotor activation, disrupted spatial behavior, moderate hyperthermia (exacerbated in group-housed animals), and transient disruption of prepulse inhibition at 4 mg/kg, consistent with a dopaminergic mechanism. No specific signs of acute toxicity were observed at the doses used.
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.
Frontiers in pharmacology
January 1, 2023
Kateřina Syrová, Klára Šíchová, Hynek Danda et al.
4 citations
2C-B-Fly-NBOMe, a new psychoactive substance related to the psychedelic entactogen 2C-B, was studied in adult male Wistar rats. After injection, peak drug levels in blood serum occurred at 30 minutes (28 ng/ml) and in brain tissue at 60 minutes (171 ng/g), with the compound still detectable in the brain after 8 hours. The drug dose-dependently reduced locomotor activity and strongly disrupted the acoustic startle response, with a weaker effect on prepulse inhibition. It did not cause significant changes in body temperature. The overall profile resembles that of 2C-B and other NBOMe substances, suggesting slow brain penetration and inhibitory effects on motor performance and sensorimotor gating.
Pharmacology, biochemistry, and behavior
June 30, 2026
Lucie Ladislavová, Viera Kútna, Kristýna Mazochová et al.
Chronic microdosing of psilocin (0.05 or 0.075 mg/kg) in adult male Wistar rats over five weeks did not alter locomotor activity, depressive-like behavior, sociability, or novelty seeking, and did not increase cell proliferation in the dentate gyrus of the hippocampus. A small anxiogenic effect was detected in the Elevated Plus Maze. The findings suggest that, under this dosing schedule, psilocin microdosing produces limited behavioral effects and does not enhance hippocampal progenitor proliferation.
Addiction Biology
March 1, 2026
Isis Koutrouli, Vojtěch Brejtr, Marek Schwendt et al.
Psilocybin and ibogaine, given in a dose-escalation protocol, facilitated extinction learning in male rats that had self-administered cocaine. Psilocybin reduced active lever pressing one day after the second dose, with a nonsignificant reduction after the first dose; ibogaine significantly reduced pressing even after the first administration. Neither drug significantly altered cue-induced reinstatement of drug-seeking, though psilocybin showed a trend toward attenuation. The treatments had no side effects on general locomotor activity or anxiety-like behavior in the open field test. These results suggest psilocybin and ibogaine may support extinction learning and possibly protect against relapse, warranting further research into their antiaddictive potential.