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
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Comparative Study
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Benzodioxoles / chemistry
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Benzodioxoles / pharmacology*
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Central Nervous System Stimulants / chemistry
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Central Nervous System Stimulants / pharmacology*
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Designer Drugs / chemistry
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Designer Drugs / pharmacology*
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Dopamine Plasma Membrane Transport Proteins / genetics
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Dopamine Plasma Membrane Transport Proteins / metabolism*
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Dose-Response Relationship, Drug
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Humans
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In Vitro Techniques
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Membrane Potentials / drug effects
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Methamphetamine / analogs & derivatives*
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Methamphetamine / chemistry
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Methamphetamine / pharmacology
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Molecular Structure
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Oocytes / metabolism
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Patch-Clamp Techniques
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Pyrrolidines / chemistry
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Pyrrolidines / pharmacology*
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Structure-Activity Relationship
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Synaptic Transmission / drug effects
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Synthetic Cathinone
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Transfection
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Xenopus laevis
Substances
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Benzodioxoles
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Central Nervous System Stimulants
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Designer Drugs
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Dopamine Plasma Membrane Transport Proteins
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Pyrrolidines
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Methamphetamine
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mephedrone
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Synthetic Cathinone