[18F]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO)
[18F]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO)
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DOI：
10.1016/j.bmcl.2011.12.084
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发表时间：
2012-02-01
影响因子：
2.7
通讯作者：
Trigg, William
中科院分区：
文献类型：
--
作者：
Wadsworth, Harry;Jones, Paul A.;Trigg, William
已经合成了一系列三环化合物，并在体外评估了对转运蛋白18 kDa（TSPO）的亲和力和优选的成像特性。对最有前途的化合物进行放射性标记并进行体内评价，以确定高表达TSPO区域的生物分布和特异性。还研究了脑和血浆中的代谢物谱。还在神经炎症的放射自显影模型中对最佳化合物12 a（[F-18]GE-180）进行了评价。(C)2011爱思唯尔有限公司保留所有权利。
A series of tricyclic compounds have been synthesised and evaluated in vitro for affinity against Translocator protein 18 kDa (TSPO) and for preferred imaging properties. The most promising of the compounds were radiolabelled and evaluated in vivo to determine biodistribution and specificity for high expressing TSPO regions. Metabolite profiling in brain and plasma was also investigated. Evaluation in an autoradiography model of neuroinflammation was also carried out for the best compound, 12a ([F-18]GE-180). (C) 2011 Elsevier Ltd. All rights reserved.