In vivo binding of [3H]GBR 12783, a selective dopamine uptake inhibitor, in mouse striatum.

[3H]GBR 12783 (1,2-(diphenylmethoxy)ethyl-4-(3-phenyl-2-propenyl)-piperazine), a specific dopamine uptake inhibitor, was tested for in vivo central binding in mice. The difference between the striatal and cerebellar levels of radioactivity was maximal 1 hour after the i.v. injection of a tracer dose of [3H]GBR 12783. The additional accumulation of radioactivity in striatum, relatively to cerebellum, was dose-dependently decreased by dopamine uptake inhibitors. It was unaffected by high doses of dopamine receptor agonists or antagonists and of serotonin or norepinephrine uptake blockers. The intrastriatal injection of 6-hydroxydopamine (6-OHDA) resulted in an almost similar decrease in both the synaptosomal [3H]dopamine uptake and the in vivo [3H]GBR 12783 binding. These data suggest that [3H]GBR 12783 injected i.v. labels the dopamine transport complex in the striatum and thus can be used for the in vivo assessment of the density of dopaminergic nerve endings in brain areas.