ArticleBritish journal of pharmacology2013
Bath salts components mephedrone and methylenedioxypyrovalerone (MDPV) act synergistically at the human dopamine transporter.
Article in British journal of pharmacology, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 65 papers.
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Who cites it
65 citing papers in PubMed, 107 citations in OpenAlex.
- Structural and functional perspectives on interactions between synthetic cathinones and monoamine transporters.Advances in pharmacology (San Diego, Calif.) · 2024Article
- Structure-Activity Relationships for a Recently Controlled Synthetic Cathinone Dopamine Transporter Reuptake Inhibitor: α-Pyrrolidinohexiophenone (α-PHP).ACS chemical neuroscience · 2023Article
- An Update on the Implications of New Psychoactive Substances in Public Health.International journal of environmental research and public health · 2022Review
- Non-conserved residues dictate dopamine transporter selectivity for the potent synthetic cathinone and psychostimulant MDPV.Neuropharmacology · 2021Article
- An updated review on synthetic cathinones.Archives of toxicology · 2021Review
- Acute MDPV Binge Paradigm on Mice Emotional Behavior and Glial Signature.Pharmaceuticals (Basel, Switzerland) · 2021Article
- Substance-Induced Psychoses: An Updated Literature Review.Frontiers in psychiatry · 2021Review
- Detrimental effects of the 'bath salt' methylenedioxypyrovalerone on social play behavior in male rats.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020Article
- 3,4-Methylenedioxypyrovalerone: Neuropharmacological Impact of a Designer Stimulant of Abuse on Monoamine Transporters.The Journal of pharmacology and experimental therapeutics · 2020Article
- Combined effects of mephedrone and cocaine on locomotor activity and conditioned place preference in male Sprague-Dawley rats.Behavioural pharmacology · 2020Article
- Abuse potential and toxicity of the synthetic cathinones (i.e., "Bath salts").Neuroscience and biobehavioral reviews · 2020Review
- Cell-Based Radiotracer Binding and Uptake Inhibition Assays: A Comparison ofFrontiers in pharmacology · 2020Article
- The psychoactive cathinone derivative pyrovalerone alters locomotor activity and decreases dopamine receptor expression in zebrafish (Danio rerio).Brain and behavior · 2019Article
- Dopaminergic Effects of Major Bath Salt Constituents 3,4-Methylenedioxypyrovalerone (MDPV), Mephedrone, and Methylone Are Enhanced Following Co-exposure.Neurotoxicity research · 2019Article
- Is the 3,4-methylendioxypyrovalerone/mephedrone combination responsible for enhanced stimulant effects? A rat study with investigation of the effect/concentration relationships.Psychopharmacology · 2019Article
- Contribution of monoaminergic mechanisms to the discriminative stimulus effects of 3,4-methylenedioxypyrovalerone (MDPV) in Sprague-Dawley rats.Psychopharmacology · 2019Article
- Using CaPsychopharmacology · 2019Review
- The synthetic cathinones, butylone and pentylone, are stimulants that act as dopamine transporter blockers but 5-HT transporter substrates.Psychopharmacology · 2019Article
- Raman Spectroscopic Analysis of Signaling Molecules-Dopamine Receptors Interactions in Living Cells.ACS omega · 2018Article
- DARK Classics in Chemical Neuroscience: Cathinone-Derived Psychostimulants.ACS chemical neuroscience · 2018Review
5 more citing papers are in PubMed but not listed here.
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeBath salts is the street name for drug combinations that contain synthetic cathinone analogues, among them possibly mephedrone (MEPH) and certainly methylenedioxypyrovalerone (MDPV). In animal studies, cathinone and certain cathinone analogues release dopamine (DA), similar to the action of amphetamine (AMPH) and methamphetamine (METH). AMPH and METH act on the human DA transporter (hDAT); thus, we investigated MEPH and MDPV acting at hDAT. EXPERIMENTAL APPROACH: We recorded electrical currents mediated by hDAT expressed in Xenopus laevis oocytes and exposed to: DA, METH, a known hDAT stimulant and DA releaser, MEPH, MDPV, MEPH + MDPV, or cocaine, a known hDAT inhibitor. KEY
resultsDA, METH and MEPH induce an inward current (depolarizing) when the oocyte is held near the resting potential (-60 mV), therefore acting as excitatory hDAT substrates. Structurally analogous MDPV induces an outward (hyperpolarizing) current similar to cocaine, therefore acting as an inhibitory non-substrate blocker. CONCLUSIONS AND IMPLICATIONS: Two components of bath salts, MEPH and MDPV, produce opposite effects at hDAT that are comparable with METH and cocaine, respectively. In our assay, MEPH is nearly as potent as METH; however, MDPV is much more potent than cocaine and its effect is longer lasting. When applied in combination, MEPH exhibits faster kinetics than MDPV, viz., the MEPH depolarizing current occurs seconds before the slower MDPV hyperpolarizing current. Bath salts containing MEPH (or a similar drug) and MDPV might then be expected initially to release DA and subsequently prevent its reuptake via hDAT. Such combined action possibly underlies some of the reported effects of bath salts abuse.
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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.