[The effect of the dopamine neuronal reuptake inhibitor GBR 12909 on the dopaminergic neurotransmission parameters in the rat striatum in vivo].
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.
Budygin
E A
EA
Department of Chemistry, University of North Carolina, Chapel Hill, USA.
Kilpatrick
M
M
Gaĭnetdinov
R R
RR
Raevskiĭ
K S
KS
Wightman
R M
RM
D000818:Animals; D065105:Aromatic Amino Acid Decarboxylase Inhibitors; D003342:Corpus Striatum / Q000187:drug effects* / Q000502:physiology; D004298:Dopamine / Q000378:metabolism; D018765:Dopamine Uptake Inhibitors / Q000008:administration & dosage / Q000494:pharmacology*; D004347:Drug Interactions; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006834:Hydrazines / Q000494:pharmacology; D007980:Levodopa / Q000378:metabolism; D008297:Male; D017551:Microdialysis; D009474:Neurons / Q000187:drug effects* / Q000502:physiology; D010879:Piperazines / Q000008:administration & dosage / Q000494:pharmacology*; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects* / Q000502:physiology; D009435:Synaptic Transmission / Q000187:drug effects* / Q000502:physiology
D065105:Aromatic Amino Acid Decarboxylase Inhibitors; D018765:Dopamine Uptake Inhibitors; D004791:Enzyme Inhibitors; D006834:Hydrazines; D010879:Piperazines; D011954:Receptors, Dopamine; D007980:Levodopa; C043425:vanoxerine; C004297:3-hydroxybenzylhydrazine; D004298:Dopamine