Kuhar M J, Sanchez-Roa P M, Wong D F, Dannals R F, Grigoriadis D E, Lew R, Milberger M
Neuroscience Branch, National Institute on Drug Abuse, Baltimore, Md.
Eur Neurol. 1990;30 Suppl 1:15-20. doi: 10.1159/000117169.
In recent years, there has been substantial progress in studying the dopamine transporter, a unique component of the functioning dopaminergic nerve terminal. The transporter has been studied by direct binding techniques using a variety of ligands which function as inhibitors of transport. Analogues of these ligands have been used as photoaffinity labels to solubilize and further characterize the transporter. While a variety of drugs bind to the transporter, it is clear that the transporter may serve as an important drug receptor, particularly for the reinforcing properties of some psychostimulants such as cocaine. An extension of the in vitro ligand-binding studies reveals that it is possible to preferentially label the transporter in vivo. The success of in vivo labeling has lead to successful positron emission tomographic scanning studies of the transporter. These studies in turn have revealed the usefulness of imaging the transporter, a measure of the presence of dopaminergic nerve terminals, as a potential diagnostic tool in Parkinson's disease.
近年来，在研究多巴胺转运体方面取得了重大进展，多巴胺转运体是功能性多巴胺能神经末梢的独特组成部分。通过使用多种作为转运抑制剂的配体的直接结合技术对该转运体进行了研究。这些配体的类似物已被用作光亲和标记物，以溶解并进一步表征该转运体。虽然多种药物与该转运体结合，但很明显该转运体可能作为一种重要的药物受体，特别是对于某些精神兴奋剂如可卡因的强化特性而言。体外配体结合研究的扩展表明，有可能在体内优先标记该转运体。体内标记的成功导致了对该转运体的成功正电子发射断层扫描研究。这些研究反过来又揭示了对该转运体进行成像的有用性，作为多巴胺能神经末梢存在的一种测量方法，可作为帕金森病的一种潜在诊断工具。
