Costentin J
Unité de Neuropsychopharmacologie Expérimentale, C.N.R.S., Faculté de Médecine & Pharmacie de Rouen, Saint-Etienne-du-Rouvray.
Ann Pharm Fr. 1995;53(4):145-54.
The dopamine carrier (dopamine uptake complex) is located on the membrane of dopaminergic neurons in a diffuse pattern. It is involved in the uptake of the dopamine released into the synaptic cleft. Considered at the level of nigro-striatal dopaminergic neurons, whose degeneration is responsible for the Parkinson's disease, this carrier seems to constitute a major target. It could be involved in the nigro-striatal neurodegeneration by concentrating neurotoxins. Its in vivo labelling by position emitting agents should allow evidencing of a partial striatal dopaminergic denervation, before the occurrence of extrapyramidal troubles. Its blockable by pure dopamine uptake inhibitors, by preventing the neuronal concentration of toxins, could stop the neurodegeneration process. These agents by inhibiting the dopamine reuptake, could also lessen extrapyramidal troubles as well as the depressive manifestations which are frequently associated to Parkinson's disease.
多巴胺载体(多巴胺摄取复合体)以弥散的方式位于多巴胺能神经元的膜上。它参与摄取释放到突触间隙中的多巴胺。在黑质 - 纹状体多巴胺能神经元层面考虑,其退化是帕金森病的病因,这种载体似乎构成一个主要靶点。它可能通过浓缩神经毒素参与黑质 - 纹状体神经变性。通过发射性定位剂对其进行体内标记,应能在锥体外系症状出现之前证实部分纹状体多巴胺能去神经支配。通过防止神经元毒素浓度升高,其可被纯多巴胺摄取抑制剂阻断,从而可能阻止神经变性过程。这些药物通过抑制多巴胺再摄取,还可减轻锥体外系症状以及帕金森病常伴发的抑郁表现。