ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2012
The designer methcathinone analogs, mephedrone and methylone, are substrates for monoamine transporters in brain tissue.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 237 papers, 1 of them a synthesis that pooled it.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
237 citing papers in PubMed, 1 synthesis or guideline pooled it, 434 citations in OpenAlex.
- A systematic review and meta-analysis of synthetic cathinone use and psychosis.Psychopharmacology · 2024Pooled it
- Efficacy and Safety of the Neuroplastogen TSND-201 for the Treatment of PTSD: A Randomized Clinical Trial.JAMA psychiatry · 2026Trial
- Methylone and MDMA Pharmacokinetics Following Controlled Administration in Humans.International journal of molecular sciences · 2022Trial
- Human Pharmacology of Mephedrone in Comparison with MDMA.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2016Trial
- αMolecular psychiatry · 2026Article
- Alkyl-Chain Extension and Terminal Amine Substitution Shape Cardiotoxic Profiles of Methylenedioxy Cathinones in Zebrafish Embryos.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Untangling Mephedrone-Induced Social Reward in Rats-The Involvement of Oxytocin and Vasopressin VGenes, brain, and behavior · 2026Article
- Effects of psychostimulants on locomotor activity in the BTBR TPsychopharmacology · 2026Article
- TRACT assay-based in vitro characterization of substituted cathinones: inhibition and release at the serotonin transporter.Archives of toxicology · 2026Article
- Methylone promotes neurite outgrowth and has long-lasting effects on fear extinction learning.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2026Article
- Locomotor and discriminative stimulus effects of N-cyclohexyl butylone and N-cyclohexyl methylone.Frontiers in pharmacology · 2026Article
- Discriminating evidence - use and misuse of the drug-discrimination test in abuse potential assessment of novel CNS drugs.Journal of psychopharmacology (Oxford, England) · 2025Review
- Cell-Specific Vulnerability of Human Glioblastoma and Astrocytoma Cells to Mephedrone-An In Vitro Study.Molecules (Basel, Switzerland) · 2025Article
- Structure-Activity Relationship of Synthetic Cathinones: An Updated Review.ACS pharmacology & translational science · 2024Review
- Bioisosteric analogs of MDMA: Improving the pharmacological profile?Journal of neurochemistry · 2024Article
- Opposite Contractile Effects of Amphetamine-Related Hallucinogenic Drugs in the Isolated Human Atrium.International journal of molecular sciences · 2024Article
- Effects of congeners of amphetamine on the human heart.Naunyn-Schmiedeberg's archives of pharmacology · 2024Review
- The effect of mephedrone on human neuroblastoma and astrocytoma cells.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2024Article
- Synthetic Cathinones: Epidemiology, Toxicity, Potential for Abuse, and Current Public Health Perspective.Brain sciences · 2024Review
- 5-HT_FAsTR: a versatile, label-free, high-throughput, fluorescence-based microplate assay to quantify serotonin transport and release.Scientific reports · 2024Article
177 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
10 authors at 4 institutions in 2 countries.
Funding
Abstract
The nonmedical use of 'designer' cathinone analogs, such as 4-methylmethcathinone (mephedrone) and 3,4-methylenedioxymethcathinone (methylone), is increasing worldwide, yet little information is available regarding the mechanism of action for these drugs. Here, we employed in vitro and in vivo methods to compare neurobiological effects of mephedrone and methylone with those produced by the structurally related compounds, 3,4-methylenedioxymethamphetamine (MDMA) and methamphetamine. In vitro release assays using rat brain synaptosomes revealed that mephedrone and methylone are nonselective substrates for plasma membrane monoamine transporters, similar to MDMA in potency and selectivity. In vivo microdialysis in rat nucleus accumbens showed that i.v. administration of 0.3 and 1.0 mg/kg of mephedrone or methylone produces dose-related increases in extracellular dopamine and serotonin (5-HT), with the magnitude of effect on 5-HT being greater. Both methcathinone analogs were weak motor stimulants when compared with methamphetamine. Repeated administrations of mephedrone or methylone (3.0 and 10.0 mg/kg, s.c., 3 doses) caused hyperthermia but no long-term change in cortical or striatal amines, whereas similar treatment with MDMA (2.5 and 7.5 mg/kg, s.c., 3 doses) evoked robust hyperthermia and persistent depletion of cortical and striatal 5-HT. Our data demonstrate that designer methcathinone analogs are substrates for monoamine transporters, with a profile of transmitter-releasing activity comparable to MDMA. Dopaminergic effects of mephedrone and methylone may contribute to their addictive potential, but this hypothesis awaits confirmation. Given the widespread use of mephedrone and methylone, determining the consequences of repeated drug exposure warrants further study.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.