ArticleNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology2018
The abuse-related effects of pyrrolidine-containing cathinones are related to their potency and selectivity to inhibit the dopamine transporter.
Article in Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 67 papers, 1 of them a synthesis that pooled it.
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Who cites it
67 citing papers in PubMed, 1 synthesis or guideline pooled it, 93 citations in OpenAlex.
- Synthetic Cathinones and Neurotoxicity Risks: A Systematic Review.International journal of molecular sciences · 2023Pooled it
- Structure-activity relationship of synthetic cathinones: integrated in silico, in vitro, and in vivo studies of α-PiHP analogues.Archives of toxicology · 2026Article
- Exploring the addictive potential of α-methylfentanyl and acetyl-α-methylfentanyl in animal models.Psychopharmacology · 2026Article
- Neuropharmacology of levamisole and its phase I metabolites: lack of evidence for levamisole-cocaine interactions.Psychopharmacology · 2026Article
- Effects of psychostimulants on locomotor activity in the BTBR TPsychopharmacology · 2026Article
- Preclinical abuse potential testing using behavioral economics and drug self-administration demand-curve analysis: A strategy to improve resolution of drug stratification for regulatory control.Pharmacological reviews · 2026Review
- Impact of morphine dependence and withdrawal on economic demand for fentanyl, cocaine, and methamphetamine in rats.Drug and alcohol dependence · 2026Article
- Locomotor and discriminative stimulus effects of N-cyclohexyl butylone and N-cyclohexyl methylone.Frontiers in pharmacology · 2026Article
- 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
- Spectroscopic and Chromatographic Characterization of Two Isomeric Cathinone Derivatives:Molecules (Basel, Switzerland) · 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
- Unveiling the Potential Role of Cathinone and Cathine Compounds in Alzheimer's Disease: Predictive Insights.Current Alzheimer research · 2025Article
- From Psychoactivity to Antimicrobial Agents: Multifaceted Applications of Synthetic Cathinones andMolecules (Basel, Switzerland) · 2024Review
- 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
- Structure-Activity Relationship of Synthetic Cathinones: An Updated Review.ACS pharmacology & translational science · 2024Review
- Comparative Assessment of the Addictive Potential of Synthetic Cathinones by Zebrafish Conditioned Place Preference (CPP) Paradigm.Life (Basel, Switzerland) · 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
7 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 1 country.
Funding
Abstract
Synthetic cathinones are common constituents of abused "bath salts" preparations and represent a large family of structurally related compounds that function as cocaine-like inhibitors or amphetamine-like substrates of dopamine (DAT), norepinephrine (NET), and serotonin (SERT) transporters. Preclinical evidence suggests that some cathinones (e.g., MDPV and α-PVP) are more effective reinforcers than prototypical stimulant drugs of abuse, such as cocaine or methamphetamine. Although the reinforcing potency of these cathinones is related to their potency to inhibit DAT, less is known about the pharmacological determinants of their unusually high reinforcing effectiveness. To this end, we tested the hypothesis that reinforcing effectiveness of cathinone stimulants is positively correlated with their selectivity for DAT relative to SERT. Uptake inhibition assays in rat brain synaptosomes were used to directly compare the potency of MDPV, MDPBP, MDPPP, α-PVP, α-PPP, and cocaine at DAT, NET, and SERT, whereas intravenous self-administration in rats was used to quantify relative reinforcing effectiveness of the drugs using progressive ratio (PR) and behavioral economic procedures. All cathinones were more potent at DAT than NET or SERT, with a rank order for selectivity at DAT over SERT of α-PVP > α-PPP > MDPV > MDPBP > MDPPP > cocaine. These synthetic cathinones were more effective reinforcers than cocaine, and the measures of reinforcing effectiveness determined by PR and demand curve analyses were highly correlated with selectivity for DAT over SERT. Together, these studies provide strong and convergent evidence that the abuse potential of stimulant drugs is mediated by uptake inhibition at DAT, with activity at SERT serving as a negative modulator of reinforcing effectiveness.
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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.