Summary.
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 [3H]dopamine uptake in a competitive and dose-dependent manner and had no effect on [3H]dihydrotetrabenazine binding. At higher concentrations the drugs enhanced [3H]dopamine vesicular efflux. Parachloroamphetamine was the most potent agent while methylendioxymethamphetamine was the weakest one. The vesicular activities may be relevant to their neurotoxicity.
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Schwartz, K., Weizman, A. & Rehavi, M. The effect of psychostimulants on [3H]dopamine uptake and release in rat brain synaptic vesicles. J Neural Transm 113, 1347–1352 (2006). https://doi.org/10.1007/s00702-005-0383-4
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DOI: https://doi.org/10.1007/s00702-005-0383-4