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


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.
Department of Physiology and Biophysics, School of Medicine, Virginia Commonwealth University, Richmond, VA 23298, USA.
Krasnodara
K
Cameron
Renata
R
Kolanos
Rakesh
R
Vekariya
Rakesh
R
Verkariya
Louis
L
De Felice
Richard A
RA
Glennon
D000818:Animals; D052117:Benzodioxoles / Q000737:chemistry / Q000494:pharmacology*; D000697:Central Nervous System Stimulants / Q000737:chemistry / Q000494:pharmacology*; D015198:Designer Drugs / Q000737:chemistry / Q000494:pharmacology*; D050483:Dopamine Plasma Membrane Transport Proteins / Q000235:genetics / Q000378:metabolism*; D004305:Dose-Response Relationship, Drug; D006801:Humans; D066298:In Vitro Techniques; D008564:Membrane Potentials / Q000187:drug effects; D008694:Methamphetamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D009865:Oocytes / Q000378:metabolism; D018408:Patch-Clamp Techniques; D011759:Pyrrolidines / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D009435:Synaptic Transmission / Q000187:drug effects; D014162:Transfection; D014982:Xenopus laevis; D000094982:Synthetic Cathinone
D052117:Benzodioxoles; D000697:Central Nervous System Stimulants; D015198:Designer Drugs; D050483:Dopamine Plasma Membrane Transport Proteins; D011759:Pyrrolidines; D008694:Methamphetamine; C548233:mephedrone; D000094982:Synthetic Cathinone