[18F]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18 kDa (TSPO)

被引：99

作者：

Wadsworth, Harry ^{[1
]}

Jones, Paul A. ^{[1
]}

Chau, Wai-Fung ^{[1
]}

Durrant, Clare ^{[1
]}

Fouladi, Naghmeh ^{[1
]}

Passmore, Joanna ^{[1
]}

O'Shea, Dennis ^{[1
]}

Wynn, Duncan ^{[1
]}

Morisson-Iveson, Veronique ^{[1
]}

Ewan, Amanda ^{[1
]}

Thaning, Mikkel ^{[2
]}

Mantzilas, Dimitrios ^{[2
]}

Gausemel, Ingvil ^{[2
]}

Khan, Imtiaz ^{[1
]}

Black, Andrew ^{[1
]}

Avory, Michelle ^{[1
]}

Trigg, William ^{[1
]}

机构：

[1] GE Healthcare, Grove Ctr, Amersham HP9 7LL, Bucks, England

[2] GE Healthcare AS, N-0401 Oslo, Norway

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2012年 / 22卷 / 03期

关键词：

TSPO; PBR; PET; Neuroinflammation; Radiosynthesis; PERIPHERAL BENZODIAZEPINE-RECEPTORS; LIGANDS; BRAIN; CHROMATOGRAPHY; BINDING;

D O I：

10.1016/j.bmcl.2011.12.084

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：1308 / 1313

页数：6

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