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.
- Vesicular Monoamine Transporter (VMAT2)