The effect of the dopamine neuronal reuptake inhibitor GBR 12909 on the dopaminergic neurotransmission parameters in the rat striatum in vivo
Budygin EA, Kilpatrick M, Gainetdinov RR, Raevskii KS, Wightman RM
Department of Chemistry,
University of North Carolina,
Chapel Hill, USA.
Eksp Klin Farmakol 1999 Sep-Oct; 62(5):3-6


The aim of the present research was to investigate the effects of the selective dopamine re-uptake inhibitor GBR 12909 (10 mg/kg, i.p.) on dopaminergic neurotransmission in rat striatum. GBR 12909 increased DA levels in microdialysis samples from freely moving rats. In contrast, administration of GBR 12909 slightly decreased the NSD 1015 (50 mg/kg)--induced DOPA accumulation. This result may be explained as a decrease in DA biosynthesis in response to an increasing amount of DA in the synaptic cleft. Fast-scan cyclic voltammetric monitoring of electrically-evoked DA showed significant changes after the drug in DA re-uptake (Km), but not DA release. In conclusion, our results support the notion, that GBR 12909 is a specific DA uptake inhibitor without any transmitter releasing action.

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