title: The effect of psychostimulants on [3H]dopamine uptake and release in rat brain synaptic vesicles.
abstract: Amphetamine and its derivatives are psychostimulants active at the plasma membrane monoamine transporters. In the present study we assessed the interaction of parachloroamphetamine, D-amphetamine, fenfluramine and methylendioxymethamphetamine with brain vesicular monoamine transporter using purified rat striatal synaptic vesicles. All four psychostimulants inhibited vesicular [(3)H]dopamine uptake in a competitive and dose-dependent manner and had no effect on [(3)H]dihydrotetrabenazine binding. At higher concentrations the drugs enhanced [(3)H]dopamine vesicular efflux. Parachloroamphetamine was the most potent agent while methylendioxymethamphetamine was the weakest one. The vesicular activities may be relevant to their neurotoxicity.
authors.affiliation: Department of Physiology and Pharmacology, Sackler Faculty of Medicine, Tel Aviv University, Tel Aviv, Israel.
authors.forename: K
authors.initials: K
authors.lastname: Schwartz
authors.forename: A
authors.initials: A
authors.lastname: Weizman
authors.forename: M
authors.initials: M
authors.lastname: Rehavi
mesh_terms: D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D000697:Central Nervous System Stimulants / Q000494:pharmacology*; D004298:Dopamine / Q000378:metabolism*; D018765:Dopamine Uptake Inhibitors; D066298:In Vitro Techniques; D007700:Kinetics; D017072:Neostriatum / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D013572:Synaptic Vesicles / Q000187:drug effects / Q000378:metabolism*; D050493:Vesicular Monoamine Transport Proteins / Q000378:metabolism*
chemical_list: D000697:Central Nervous System Stimulants; D018765:Dopamine Uptake Inhibitors; C493454:Slc18a2 protein, rat; D050493:Vesicular Monoamine Transport Proteins; D004298:Dopamine