摘要
本文对多巴胺转运蛋白(DAT)抑制剂的药理研究综述,该抑制剂是治疗神经退行性疾病和精神疾病的潜在方法。广泛的构效关系研究发现莨菪烷基配体对DAT具有高度选择性,对DAT和其他单胺转运体(如双单胺和三单胺再摄取抑制剂)具有亲和性。本文总结了过去十五年该领域的研究进展。所述化合物中,许多是有前景的候选药物,而其他化合物可作为有价值的研究工具或作为新型选择性DAT抑制剂的原型。本文特别强调了从NET和SERT抑制剂中对DAT抑制剂的分离。
关键词: 可卡因滥用,抑郁症,多动症,多巴胺转运蛋白抑制剂,单胺转运体抑制剂,莨菪烷衍生物。
Current Medicinal Chemistry
Title:Progress in the Search for New Dopamine Transporter Inhibitors
Volume: 22 Issue: 28
Author(s): Beata Gryzlo, Paula Zareba, Katarzyna Malawska, Anna Jakubowska and Katarzyna Kulig
Affiliation:
关键词: 可卡因滥用,抑郁症,多动症,多巴胺转运蛋白抑制剂,单胺转运体抑制剂,莨菪烷衍生物。
摘要: In the present review, we provide a comprehensive summary of recent pharmacological studies on dopamine transporter (DAT) inhibitors, which are potential treatments for neurodegenerative and psychiatric disorders. Extensive structure-activity relationship studies have identified numerous tropane-based ligands with high affinity and selectivity for the DAT or with high affinity to the DAT and other monoamine transporters (dual and triple monoamine reuptake inhibitors). The review covers advances in the field in past fifteen years. Among the described compounds, many appear to be promising drug candidates, while other may serve as valuable tools for research or as prototypes for new classes of selective DAT inhibitors. Special attention is being paid to separation of the DAT inhibition from NET and SERT inhibition.
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Beata Gryzlo, Paula Zareba, Katarzyna Malawska, Anna Jakubowska and Katarzyna Kulig , Progress in the Search for New Dopamine Transporter Inhibitors, Current Medicinal Chemistry 2015; 22 (28) . https://dx.doi.org/10.2174/0929867322666150812145631
DOI https://dx.doi.org/10.2174/0929867322666150812145631 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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