Evidence map›Paper›PMID 27830575›Full record

ReviewCurrent topics in behavioral neurosciences2017

Neuropharmacology of 3,4-Methylenedioxypyrovalerone (MDPV), Its Metabolites, and Related Analogs.

Michael H Baumann, Mohammad O Bukhari, Kurt R Lehner, Sebastien Anizan, Kenner C Rice, Marta Concheiro, Marilyn A Huestis

Open access · hybridAbstract readReview
In one paragraph

Review in Current topics in behavioral neurosciences, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 47 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
47citing papers in PubMed, 1 pooled it
22.3field-weighted citation impact, top 1% of its field
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

47 citing papers in PubMed, 1 synthesis or guideline pooled it, 128 citations in OpenAlex.

  1. Pooled it
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  8. Persistent binding at dopamine transporters determines sustained psychostimulant effects.Proceedings of the National Academy of Sciences of the United States of America · 2023
    Article
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  13. An updated review on synthetic cathinones.Archives of toxicology · 2021
    Review
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  19. Detrimental effects of the 'bath salt' methylenedioxypyrovalerone on social play behavior in male rats.Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology · 2020
    Article
  20. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors at 2 institutions in 1 country.

Michael H BaumannDesigner Drug Research Unit of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA. mbaumann@mail.nih.gov.
Mohammad O BukhariDesigner Drug Research Unit of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
Kurt R LehnerDesigner Drug Research Unit of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
Sebastien AnizanChemistry and Drug Metabolism Section of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
Kenner C RiceDrug Design and Synthesis Section of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
Marta ConcheiroChemistry and Drug Metabolism Section of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
Marilyn A HuestisChemistry and Drug Metabolism Section of the Intramural Research Program, National Institute on Drug Abuse (NIDA), National Institutes of Health, Baltimore, MD, USA.
National Institute on Drug Abuse · USNational Institutes of Health · US

Funding

Studies on MDMA and Related CompoundsZIADA000523 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI BAUMANN, MICHAEL · 2009 to 2025
$16.4M
Medicinal Chemistry of Drugs Acting on Biogenic Amine ReceptorsZIADA000532 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI RICE, KENNER · 2009 to 2020
$4.5M
Intramural NIH HHS ZIA DA000523
6 · The paper itself

Abstract

3,4-Methylenedioxypyrovalerone (MDPV) is a psychoactive component of so-called bath salts products that has caused serious medical consequences in humans. In this chapter, we review the neuropharmacology of MDPV and related analogs, and supplement the discussion with new results from our preclinical experiments. MDPV acts as a potent uptake inhibitor at plasma membrane transporters for dopamine (DAT) and norepinephrine (NET) in nervous tissue. The MDPV formulation in bath salts is a racemic mixture, and the S isomer is much more potent than the R isomer at blocking DAT and producing abuse-related effects. Elevations in brain extracellular dopamine produced by MDPV are likely to underlie its locomotor stimulant and addictive properties. MDPV displays rapid pharmacokinetics when injected into rats (0.5-2.0 mg/kg), with peak plasma concentrations achieved by 10-20 min and declining quickly thereafter. MDPV is metabolized to 3,4-dihydroxypyrovalerone (3,4-catechol-PV) and 4-hydroxy-3-methoxypyrovalerone (4-OH-3-MeO-PV) in vivo, but motor activation produced by the drug is positively correlated with plasma concentrations of parent drug and not its metabolites. 3,4-Catechol-PV is a potent uptake blocker at DAT in vitro but has little activity after administration in vivo. 4-OH-3-MeO-PV is the main MDPV metabolite but is weak at DAT and NET. MDPV analogs, such as α-pyrrolidinovalerophenone (α-PVP), display similar ability to inhibit DAT and increase extracellular dopamine concentrations. Taken together, these findings demonstrate that MDPV and its analogs represent a unique class of transporter inhibitors with a high propensity for abuse and addiction.

Indexed as

Adrenergic Uptake InhibitorsAnimalsBehavior, AnimalBenzodioxolesBrainDopamine Plasma Membrane Transport ProteinsDopamine Uptake InhibitorsHumansNeuropharmacologyNorepinephrine Plasma Membrane Transport ProteinsPsychotropic DrugsPyrrolidinesSubstance-Related DisordersSynthetic CathinoneAdrenergic Uptake Inhibitorsalpha-pyrrolidinovalerophenoneBenzodioxolesDopamine Plasma Membrane Transport ProteinsDopamine Uptake InhibitorsNorepinephrine Plasma Membrane Transport ProteinsPsychotropic DrugsPyrrolidinesSynthetic CathinoneAddictionDopamineMDPVPyrrolidinophenonesSynthetic cathinonesTransporterUptakeα-PVP

Identifiers

PMID27830575
PMCPMC5392131
OpenAlexW2551821836

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.