ArticlePsychopharmacology2019
The synthetic cathinones, butylone and pentylone, are stimulants that act as dopamine transporter blockers but 5-HT transporter substrates.
Article in Psychopharmacology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers, 1 of them a synthesis that pooled it.
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Who cites it
14 citing papers in PubMed, 1 synthesis or guideline pooled it, 30 citations in OpenAlex.
- Synthetic Cathinones and Neurotoxicity Risks: A Systematic Review.International journal of molecular sciences · 2023Pooled it
- Alkyl-Chain Extension and Terminal Amine Substitution Shape Cardiotoxic Profiles of Methylenedioxy Cathinones in Zebrafish Embryos.Pharmaceuticals (Basel, Switzerland) · 2026Article
- Prolintane analogs as hybrid monoamine transporter ligands: Structural determinants and species differences.The Journal of biological chemistry · 2025Article
- EMCDDA framework and practical guidance for naming cathinones.Drug testing and analysis · 2024Article
- Novel Benzofuran Derivatives Induce Monoamine Release and Substitute for the Discriminative Stimulus Effects of 3,4-Methylenedioxymethamphetamine.The Journal of pharmacology and experimental therapeutics · 2024Article
- Effects of Serial Polydrug Use on the Rewarding and Aversive Effects of the Novel Synthetic Cathinone Eutylone.Brain sciences · 2023Article
- Eutylone and Its Structural Isomers Interact with Monoamine Transporters and Induce Locomotor Stimulation.ACS chemical neuroscience · 2021Article
- Psychoactive Drugs-From Chemical Structure to Oxidative Stress Related to Dopaminergic Neurotransmission. A Review.Antioxidants (Basel, Switzerland) · 2021Review
- Self-Administration of Entactogen Psychostimulants Dysregulates Gamma-Aminobutyric Acid (GABA) and Kappa Opioid Receptor Signaling in the Central Nucleus of the Amygdala of Female Wistar Rats.Frontiers in behavioral neuroscience · 2021Article
- Structure-Activity Relationship of Novel Second-Generation Synthetic Cathinones: Mechanism of Action, Locomotion, Reward, and Immediate-Early Genes.Frontiers in pharmacology · 2021Article
- Synthetic Cathinones Induce Cell Death in Dopaminergic SH-SY5Y Cells via Stimulating Mitochondrial Dysfunction.International journal of molecular sciences · 2020Article
- Seizures of illicit substances for personal use in two Italian provinces: analysis of trends by type and purity from 2008 to 2017.Substance abuse treatment, prevention, and policy · 2019Article
- Locomotor activity and discriminative stimulus effects of five novel synthetic cathinone analogs in mice and rats.Drug and alcohol dependence · 2019Article
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Authors and funding
9 authors at 5 institutions in 3 countries.
Funding
Abstract
rationaleSynthetic cathinones continue to emerge in recreational drug markets worldwide. 1-(1,3-Benzodioxol-5-yl)-2-(methylamino)butan-1-one (butylone) and 1-(1,3-benzodioxol-5-yl)-2-(methylamino)pentan-1-one (pentylone) are derivatives of the cathinone compound, 1-(1,3-benzodioxol-5-yl)-2-(methylamino)propan-1-one (methylone), that are being detected in drug products and human casework.
objectivesThe purpose of the present study was to examine the neuropharmacology of butylone and pentylone using in vitro and in vivo methods.
methodsIn vitro uptake and release assays were carried out in rat brain synaptosomes and in cells expressing human dopamine transporters (DAT) and 5-HT transporters (SERT). In vivo microdialysis was performed in the nucleus accumbens of conscious rats to assess drug-induced changes in neurochemistry.
resultsButylone and pentylone were efficacious uptake blockers at DAT and SERT, though pentylone was more DAT-selective. Both drugs acted as transporter substrates that evoked release of [
conclusionsOur data demonstrate that increasing the α-carbon chain length of methylone creates "hybrid" transporter compounds which act as DAT blockers but SERT substrates. Nevertheless, butylone and pentylone elevate extracellular dopamine and stimulate motor activity, suggesting both drugs possess significant risk for abuse.
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