ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2013
Powerful cocaine-like actions of 3,4-methylenedioxypyrovalerone (MDPV), a principal constituent of psychoactive 'bath salts' products.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 229 papers, 1 of them a synthesis that pooled it.
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Who cites it
229 citing papers in PubMed, 1 synthesis or guideline pooled it, 412 citations in OpenAlex.
- Exploring the Impact of Chirality of Synthetic Cannabinoids and Cathinones: A Systematic Review on Enantioresolution Methods and Enantioselectivity Studies.International journal of molecular sciences · 2025Pooled it
- Structure-activity relationship of synthetic cathinones: integrated in silico, in vitro, and in vivo studies of α-PiHP analogues.Archives of toxicology · 2026Article
- Pharmacological characterization of 4-F-3-Me-α-PVP: A novel synthetic cathinone with psychostimulant effects and abuse liability in rodents.Journal of psychopharmacology (Oxford, England) · 2026Article
- Effects of psychostimulants on locomotor activity in the BTBR TPsychopharmacology · 2026Article
- Comprehensive metabolic profiling of the new designer stimulant MDPiHP-in vitro and in vivo identification of potential biomarkers for detection in human samples.Analytical and bioanalytical chemistry · 2026Article
- Treatment with rapamycin prevents induction and expression of locomotor sensitization to synthetic cathinone 3,4-methylenedioxypyrovalerone (MDPV) in mice.Forensic toxicology · 2026Article
- Integrated Assessment of the Cardiotoxic and Neurobehavioral Effects of 3,4-Methylenedioxypyrovalerone (MDPV) in Zebrafish Embryos.International journal of molecular sciences · 2025Article
- Prolintane analogs as hybrid monoamine transporter ligands: Structural determinants and species differences.The Journal of biological chemistry · 2025Article
- Methamphetamine and α-pyrrolidinopentiophenone (α-PVP) intravenous self-administration in female and male rats.Psychopharmacology · 2025Article
- Methamphetamine and α-pyrrolidinopentiophenone (α-PVP) Intravenous Self-Administration in Female and Male Rats.bioRxiv : the preprint server for biology · 2025Article
- Polydrug fatal intoxication involving MDPHP: Detection and in silico investigation of multiple 3,4-methylenedioxy-derived designer drugs and their metabolites.Journal of analytical toxicology · 2025Article
- Synthesis, Characterization, and Biological Effects of Chloro-Cathinones: Toxicity and Potential Neurological Impact.International journal of molecular sciences · 2025Article
- Cardiovascular and locomotor effects of binary mixtures of common 'bath salts' constituents: Studies with methylone, methylenedioxypyrovalerone and caffeine in rats.British journal of pharmacology · 2025Article
- Access to high-fat diet results in increased sensitivity to the psychostimulant effects of MDPV in mice.Pharmacological reports : PR · 2025Article
- Unlocking the Potential of High-Quality Dopamine Transporter Pharmacological Data: Advancing Robust Machine Learning-Based QSAR Modeling.Advances in neurobiology · 2025Review
- Effects of access condition on substance use disorder-like phenotypes in male and female rats self-administering MDPV or cocaine.Drug and alcohol dependence · 2024Article
- Increases in the use of drug testing kits among nightclub and festival attendees in New York City who use ecstasy, 2017-2022.Drug and alcohol review · 2024Article
- 5-HT_FAsTR: a versatile, label-free, high-throughput, fluorescence-based microplate assay to quantify serotonin transport and release.Scientific reports · 2024Article
- Effects of access condition on substance use disorder-like phenotypes in male and female rats self-administering MDPV or cocaine.bioRxiv : the preprint server for biology · 2024Article
- Dopamine Concentration Changes Associated with the Retrodialysis of Methylone and 3,4-Methylenedioxypyrovalerone (MDPV) into the Caudate Putamen.Brain sciences · 2024Article
169 more citing papers are in PubMed but not listed here.
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Authors and funding
14 authors at 5 institutions in 3 countries.
Funding
Abstract
The abuse of psychoactive 'bath salts' containing cathinones such as 3,4-methylenedioxypyrovalerone (MDPV) is a growing public health concern, yet little is known about their pharmacology. Here, we evaluated the effects of MDPV and related drugs using molecular, cellular, and whole-animal methods. In vitro transporter assays were performed in rat brain synaptosomes and in cells expressing human transporters, while clearance of endogenous dopamine was measured by fast-scan cyclic voltammetry in mouse striatal slices. Assessments of in vivo neurochemistry, locomotor activity, and cardiovascular parameters were carried out in rats. We found that MDPV blocks uptake of [(3)H]dopamine (IC(50)=4.1 nM) and [(3)H]norepinephrine (IC(50)=26 nM) with high potency but has weak effects on uptake of [(3)H]serotonin (IC(50)=3349 nM). In contrast to other psychoactive cathinones (eg, mephedrone), MDPV is not a transporter substrate. The clearance of endogenous dopamine is inhibited by MDPV and cocaine in a similar manner, but MDPV displays greater potency and efficacy. Consistent with in vitro findings, MDPV (0.1-0.3 mg/kg, intravenous) increases extracellular concentrations of dopamine in the nucleus accumbens. Additionally, MDPV (0.1-3.0 mg/kg, subcutaneous) is at least 10 times more potent than cocaine at producing locomotor activation, tachycardia, and hypertension in rats. Our data show that MDPV is a monoamine transporter blocker with increased potency and selectivity for catecholamines when compared with cocaine. The robust stimulation of dopamine transmission by MDPV predicts serious potential for abuse and may provide a mechanism to explain the adverse effects observed in humans taking high doses of 'bath salts' preparations.
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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.