New recreational drug 1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (alpha-PVP) activates central nervous system via dopaminergic neuron
Open Access
- 1 January 2014
- journal article
- Published by Japanese Society of Toxicology in The Journal of Toxicological Sciences
- Vol. 39 (1), 1-6
- https://doi.org/10.2131/jts.39.1
Abstract
1-phenyl-2-(1-pyrrolidinyl)-1-pentanone (α-PVP) is a new designer drug of the cathinone type. People who have taken drugs containing α-PVP or other synthetic cathinone reportedly lose consciousness, develop difficulty breathing, and at worst case, die. However, the mechanism underlying α-PVP-induced neurotoxicity is unknown. The objective of the present study was to investigate the effect of α-PVP on the central nervous system (CNS) and compare its neurotoxicity with that of methamphetamine (METH) in mice. Balb/c male mice (8 weeks old) were orally administered α-PVP (25 mg/kg) or METH (5 mg/kg). α-PVP induced a significant increase in locomotor activity, which occurred earlier than locomotor activity induced by METH. This increase was inhibited by the D1 receptor antagonist SCH23990 (50 µg/kg, i.p.) and the D2 receptor antagonist sulpiride (50 mg/kg, i.m.). The extracellular concentration of dopamine (DA) in the striatum, determined by in vivo microdialysis increased immediately after α-PVP administration. These results suggest that α-PVP stimulates DA release, causing an increase in locomotor activity, and that this stimulatory effect of α-PVP on CNS is mediated, at least in part, by the D1 and D2 receptors.Keywords
This publication has 19 references indexed in Scilit:
- Analysis of Synthetic Cathinones Commonly Found in Bath Salts in Human Performance and Postmortem Toxicology: Method Development, Drug Distribution and Interpretation of ResultsJournal of Analytical Toxicology, 2013
- Long-term cognitive and neurochemical effects of “bath salt” designer drugs methylone and mephedronePharmacology Biochemistry and Behavior, 2013
- In vivo Dopamine Efflux is Decreased in Striatum of both Fragment (R6/2) and Full-Length (YAC128) Transgenic Mouse Models of Huntington's DiseaseFrontiers in Systems Neuroscience, 2011
- Analyses of second‐generation ‘legal highs’ in the UK: Initial findingsDrug Testing and Analysis, 2010
- Synthesis and Biological Evaluation of Bupropion Analogues as Potential Pharmacotherapies for Smoking CessationJournal of Medicinal Chemistry, 2010
- Enantioselective Effects of Hydroxy Metabolites of Bupropion on Behavior and on Function of Monoamine Transporters and Nicotinic ReceptorsMolecular Pharmacology, 2004
- Differential effects of stimulants on monoaminergic transporters: Pharmacological consequences and implications for neurotoxicityEuropean Journal of Pharmacology, 2000
- Inhibition of plasma membrane monoamine transporters by β-ketoamphetaminesEuropean Journal of Pharmacology, 1999
- Cathinone, a Natural AmphetamineBasic & Clinical Pharmacology & Toxicology, 1992
- Methcathinone: A new and potent amphetamine-like agentPharmacology Biochemistry and Behavior, 1987