Dopamine transporter: biochemistry, pharmacology and imaging.
Dopamine transporter: biochemistry, pharmacology and imaging.
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多巴胺转运蛋白：生物化学、药理学和成像。
DOI：
10.1159/000117169
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发表时间：
1990
影响因子：
2.4
通讯作者：
Milberger,M
中科院分区：
文献类型：
--
作者：
Kuhar,MJ;Sanchez-Roa,PM;Wong,DF;Dannals,RF;Grigoriadis,DE;Lew,R;Milberger,M
多巴胺转运体是多巴胺能神经末梢的一个独特组成部分，近年来，对多巴胺转运体的研究取得了实质性进展。通过直接结合技术研究了这种转运体，使用了多种作为转运抑制剂的配体。这些配体的类似物已被用作光亲和标记来溶解和进一步表征转运体。虽然多种药物与转运蛋白结合，但很明显，转运蛋白可能是一种重要的药物受体，特别是对于一些精神兴奋剂（如可卡因）的增强特性。体外配体结合研究的延伸表明，可以在体内优先标记转运蛋白。体内标记的成功已经导致转运体的正电子发射断层扫描研究的成功。这些研究反过来揭示了转运体成像的有用性，转运体是多巴胺能神经末端存在的测量，是帕金森病的潜在诊断工具。
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.