Reith M E, Xu C, Chen N H
Department of Biomedical and Therapeutic Sciences (formerly Basic Sciences), University of Illinois College of Medicine, Peoria 61656, USA.
Eur J Pharmacol. 1997 Apr 11;324(1):1-10. doi: 10.1016/s0014-2999(97)00065-4.
The dopamine transporter, a member of the family of Na+,Cl(-)-dependent transporters, mediates uptake of dopamine into dopaminergic neurons by an electrogenic, Na(+)- and Cl(-)-transport-coupled mechanism. Dopamine and blockers of uptake such as cocaine probably bind to both shared and separate domains on the transporter, which can be influenced dramatically by the presence of cations. Regulation of the dopamine transporter occurs both by chronic occupancy with blocker and by acute effects of D2 dopamine receptors or second messengers such as diacylglycerol (protein kinase C) and arachidonic acid. The dopamine transporter is involved in the uptake of toxins generating Parkinson's disease; it is also an important target for psychostimulant drugs, ligands for in vivo imaging and medications used for neurologic diseases involving changes in the dopamine system.
多巴胺转运体是Na⁺、Cl⁻依赖性转运体家族的成员之一，通过一种电生性的、与Na⁺和Cl⁻转运偶联的机制介导多巴胺进入多巴胺能神经元。多巴胺以及诸如可卡因等摄取阻滞剂可能会与转运体上共同的和单独的结构域结合，而阳离子的存在会对其产生显著影响。多巴胺转运体的调节既通过阻滞剂的长期占据，也通过D2多巴胺受体或第二信使如二酰基甘油（蛋白激酶C）和花生四烯酸的急性作用来实现。多巴胺转运体参与了引发帕金森病的毒素的摄取；它也是精神兴奋药物、体内成像配体以及用于治疗涉及多巴胺系统变化的神经疾病的药物的重要靶点。
