Evidence map›Paper›PMID 36082866›Full record

ArticleCurrent pharmaceutical design2022

Brain Concentrations of MDPV and its Metabolites in Male Rats: Relationship to Pharmacodynamic Effects.

Marta Concheiro, Steven Towler, Joshua S Elmore, Michael R Chojnacki, Teeshavi Acosta, Masaki Suzuki, Kenner C Rice, Michael H Baumann

Abstract read
In one paragraph

Article in Current pharmaceutical design, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
0.5field-weighted citation impact, top 42% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. 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

8 authors at 5 institutions in 2 countries.

Marta ConcheiroDepartment of Sciences, John Jay College of Criminal Justice, City University of New York, NY, USA.
Steven TowlerDepartment of Sciences, John Jay College of Criminal Justice, City University of New York, NY, USA.
Joshua S ElmoreDesigner Drug Research Unit, Intramural Research Program (IRP), National Institute on Drug Abuse (NIDA), National Institutes of Health (NIH), Baltimore, MD, USA.
Michael R ChojnackiDesigner Drug Research Unit, Intramural Research Program (IRP), National Institute on Drug Abuse (NIDA), National Institutes of Health (NIH), Baltimore, MD, USA.
Teeshavi AcostaDepartment of Sciences, John Jay College of Criminal Justice, City University of New York, NY, USA.
Masaki SuzukiDrug Design and Synthesis Section, IRP, NIDA, NIH, Rockville, MD, USA.
Kenner C RiceDrug Design and Synthesis Section, IRP, NIDA, NIH, Rockville, MD, USA.
Michael H BaumannDesigner Drug Research Unit, Intramural Research Program (IRP), National Institute on Drug Abuse (NIDA), National Institutes of Health (NIH), Baltimore, MD, USA.
John Jay College of Criminal Justice · USNational Institute on Drug Abuse · USCity University of New York · USNational Institutes of Health · USOtsuka (Japan) · JP

Funding

Studies on MDMA and Related CompoundsZIADA000523 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI BAUMANN, MICHAEL · 2009 to 2025
$16.4M
IMPROVING HEALTH CARE UTILIZATION IN HIV+ DRUG USERSK23DA000523 · NIDA · JOHNS HOPKINS UNIVERSITY · PI GEBO, KELLY A · 2001 to 2005
$794k
Studies on MDMA and Related CompoundsZ01DA000523 · NIDA · NATIONAL INSTITUTE ON DRUG ABUSE · PI ROTHMAN, RICHARD · 2008 to 2008
$199k
Intramural NIH HHS Z01 DA000523Intramural NIH HHS ZIA DA000523Intramural Research Program (IRP) of the National Institute on Drug Abuse (NIDA), NIH DA000523-13NIDA NIH HHS K23 DA000523
6 · The paper itself

Abstract

backgroundMDPV (3,4-methylenedioxypyrovalerone) is a synthetic stimulant that blocks transmitter uptake at transporters for dopamine and norepinephrine. Less is known about MDPV pharmacokinetics, especially with respect to brain concentrations of the drug and its metabolites.

objectivesThe goal of the present study was: 1) to determine brain concentrations of MDPV and its metabolites, 3,4-dihydroxypyrovalerone (3,4-catechol-PV) and 4-hydroxy-3-methoxy-pyrovalerone (4-OH-3-MeOPV), after administration of MDPV, and 2) to relate brain pharmacokinetic measures to pharmacodynamic endpoints in the same subjects.

methodsMale Sprague-Dawley rats (300-400 g) received s.c. MDPV injection (1, 2, or 4 mg/kg) or its saline vehicle. Groups of rats were decapitated at 40 min and 240 min postinjection. Locomotor behavior was rated before decapitation, and the core temperature was obtained. Plasma and frontal cortex were analyzed to quantitate MDPV and its metabolites. Striatal samples were analyzed to measure dopamine, serotonin (5-HT), and their metabolites.

resultsMDPV displayed brain-to-plasma ratios greater than 1 (range 8.8-12.1), whereas 3,4-catechol-PV and 4-OH-3-MeO-PV showed ratios less than 1 (range 0-0.3). MDPV increased behavioural scores reflective of locomotor stimulation at 40 and 240 min and produced slight hyperthermia at 240 min. MDPV had no effect on striatal dopamine but produced an increase in the metabolite homovanillic acid (HVA). Brain MDPV concentrations were positively correlated with behavioural scores and striatal HVA but not with other endpoints.

conclusionThe behavioural effects of MDPV are related to brain concentrations of the parent drug and not its metabolites. The modest effects of MDPV on monoamine systems suggest that other non-monoamine mechanisms may contribute to the effects of the drug in vivo.

Indexed as

DopamineSerotoninAnimalsBrainDose-Response Relationship, DrugHomovanillic AcidMaleNorepinephrinePyrrolidinesRatsRats, Sprague-DawleyDopamineHomovanillic AcidNorepinephrinePyrrolidinesSerotoninbrainMDPVpharmacodynamicspharmacokineticsplasmasynthetic cathinones

Identifiers

PMID36082866
PMCPMC13622999
OpenAlexW4295084164

What Socratic holds

Textmetadata
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 Socratic graph.