Abstract: | 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 μM. It also increased basal release of 3H]-dopamine from perfused rat striatal and limbic tissue in vitro at concentrations above 5 μM. Release of 3H]-dopamine from perfused rat striatal and limbic tissue stimulated with 5 μM amphetamine, was inhibited by 1 μM 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 on amphetamine-stimulated release of dopamine. |