The effect of amperozide on uptake and release of [3H]-dopamine in vitro from perfused rat striatal and limbic brain areas.

Amperozide, a putatively antipsychotic drug, was studied for its effects on uptake and release of [3H]-dopamine in rat brain in vitro. Amperozide inhibited uptake of [3H]-dopamine in striatal chopped tissue in vitro with an IC50 of 18 microM. It also increased basal release of [3H]-dopamine from perfused rat striatal and limbic tissue in vitro at concentrations above 5 microM. Release of [3H]-dopamine from perfused rat striatal and limbic tissue stimulated with 5 microM amphetamine, was inhibited by 1 microM amperozide to 46%. No significant difference was found for the effect of amperozide on in vitro release of [3H]-dopamine from corpus striatum compared to tissue from limbic brain regions; neither on basal release nor an amphetamine-stimulated release of dopamine.