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Review Article

TSPOPET配体在神经炎症成像中的基本原理和最新进展

卷 29, 期 28, 2022

发表于: 12 May, 2022

页: [4862 - 4890] 页: 29

弟呕挨: 10.2174/0929867329666220329204054

价格: $65

摘要

转位蛋白18kDa（TSPO）在外线粒体中表达，并涉及多种功能，包括胆固醇转运和类固醇生成。在正常的生理条件下，TSPO在人脑中以非常低的浓度存在，但在脑损伤和炎症的反应中显着上调。这种上调与激活的小胶质细胞密切相关。因此，TSPO特别适用于评估损伤或疾病后与脑损伤相关的活动性胶质病。三十多年来，TSPO一直作为非生物标志物进行研究。已经开发了许多靶向TSPO的正电子发射断层扫描（PET）放射性配体，用于成像大脑中的炎症进展。虽然[11C]PK11195是典型的第一代PET放射性配体，目前仍被广泛用于体内研究，主要是作为其单一更有效的R-对映异构体，但它具有严重的局限性，包括灵敏度低和定量适应性差。第二代放射性配体的特征是较高的TSPO特异性信号，但受到其他回溯的影响，例如对TSPO单核苷酸多态性（SNP）rs6971的敏感性。因此，它们在人体研究中的应用具有需要基因型受试者的负担。因此，最近的努力集中在开发改进的放射性配体上，这些配体将第二代的最佳特征与覆盖整个群体中结合亲和力差异的能力相结合。本文综述了TSPO PET配体设计和开发的重要原则，并讨论了主要化学型中的显著实例。

关键词: TSPO，神经炎症，成像，PET，放射性配体，药物开发，诊断标志物。

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