title: Bupropion, methylphenidate, and 3,4-methylenedioxypyrovalerone antagonize methamphetamine-induced efflux of dopamine according to their potencies as dopamine uptake inhibitors: implications for the treatment of methamphetamine dependence.
abstract: BACKGROUND
  Methamphetamine-abuse is a worldwide health problem for which no effective therapy is available. Inhibition of methamphetamine-induced transporter-mediated dopamine (DA) release could be a useful approach to treat methamphetamine-addiction. We assessed the potencies of bupropion, methylphenidate, and 3,4-methylenedioxypyrovalerone (MDPV) to block DA uptake or to inhibit methamphetamine-induced DA release in HEK-293 cells expressing the human DA transporter.
  
  
  RESULTS
  Bupropion, methylphenidate, and MDPV inhibited methamphetamine-induced DA release with relative potencies corresponding to their potencies to block DA uptake (potency ranks: MDPV > methylphenidate > bupropion).
  
  
  CONCLUSIONS
  Bupropion and methylphenidate antagonize the effects of methamphetamine in vitro and may be potential candidates for the treatment of stimulant addiction. However, drugs that very potently antagonize the effect of methamphetamine are likely to also exhibit considerable abuse liability (MDPV > methylphenidate > bupropion).
authors.affiliation: Psychopharmacology Research Group, Division of Clinical Pharmacology and Toxicology, Department of Biomedicine and Department of Internal Medicine, University Hospital Basel and University of Basel, Hebelstrasse 2, Basel CH-4031, Switzerland.
authors.forename: Linda D
authors.initials: LD
authors.lastname: Simmler
authors.forename: Rebecca
authors.initials: R
authors.lastname: Wandeler
authors.forename: Matthias E
authors.initials: ME
authors.lastname: Liechti
mesh_terms: D019969:Amphetamine-Related Disorders / Q000378:metabolism*; D052117:Benzodioxoles / Q000494:pharmacology*; D001692:Biological Transport; D016642:Bupropion / Q000494:pharmacology*; D004298:Dopamine / Q000378:metabolism*; D006801:Humans; D008694:Methamphetamine / Q000037:antagonists & inhibitors*; D008774:Methylphenidate / Q000494:pharmacology*; D011759:Pyrrolidines / Q000494:pharmacology*; D000094982:Synthetic Cathinone
chemical_list: D052117:Benzodioxoles; D011759:Pyrrolidines; D016642:Bupropion; D008774:Methylphenidate; D008694:Methamphetamine; D004298:Dopamine; D000094982:Synthetic Cathinone