Mephedrone and methylenedioxypyrovalerone (MDPV), major constituents of "bath salts," produce opposite effects at the human dopamine transporter

Psychopharmacology (Berl). 2013 Jun;227(3):493-9. doi: 10.1007/s00213-013-2967-2. Epub 2013 Jan 31.

Abstract

Rationale: Psychoactive "bath salts" represent a relatively new drug of abuse combination that was placed in Schedule I in October 2011. Two common ingredients of bath salts include the cathinone analogs: mephedrone and methylenedioxypyrovalerone (MDPV). The mechanism of action of these synthetic cathinone analogs has not been well investigated.

Materials and methods: Because cathinone and methcathinone are known to act as releasing agents at the human dopamine transporter (hDAT), mephedrone and MDPV were investigated at hDAT expressed in Xenopus oocytes.

Results: Whereas mephedrone was found to have the signature of a dopamine-releasing agent similar to methamphetamine or methcathinone, MDPV behaved as a cocaine-like reuptake inhibitor of dopamine.

Conclusions: Mephedrone and MDPV produce opposite electrophysiological signatures through hDAT expressed in oocytes. Implications are that the combination (as found in bath salts) might produce effects similar to a combination of methamphetamine and cocaine.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural

MeSH terms

  • Animals
  • Benzodioxoles / chemistry
  • Benzodioxoles / pharmacology*
  • Central Nervous System Stimulants / chemistry
  • Central Nervous System Stimulants / pharmacology*
  • Designer Drugs / chemistry
  • Designer Drugs / pharmacology*
  • Dopamine Plasma Membrane Transport Proteins / genetics
  • Dopamine Plasma Membrane Transport Proteins / metabolism*
  • Dose-Response Relationship, Drug
  • Humans
  • In Vitro Techniques
  • Membrane Potentials / drug effects
  • Methamphetamine / analogs & derivatives*
  • Methamphetamine / chemistry
  • Methamphetamine / pharmacology
  • Molecular Structure
  • Oocytes / metabolism
  • Patch-Clamp Techniques
  • Pyrrolidines / chemistry
  • Pyrrolidines / pharmacology*
  • Structure-Activity Relationship
  • Synaptic Transmission / drug effects
  • Synthetic Cathinone
  • Transfection
  • Xenopus laevis

Substances

  • Benzodioxoles
  • Central Nervous System Stimulants
  • Designer Drugs
  • Dopamine Plasma Membrane Transport Proteins
  • Pyrrolidines
  • Methamphetamine
  • mephedrone
  • Synthetic Cathinone