[18F]GE-180: A novel fluorine-18 labelled PET tracer for imaging Translocator protein 18kDa (TSPO)
作者:Harry Wadsworth、Paul A. Jones、Wai-Fung Chau、Clare Durrant、Naghmeh Fouladi、Joanna Passmore、Dennis O’Shea、Duncan Wynn、Veronique Morisson-Iveson、Amanda Ewan、Mikkel Thaning、Dimitrios Mantzilas、Ingvil Gausemel、Imtiaz Khan、Andrew Black、Michelle Avory、William Trigg
DOI:10.1016/j.bmcl.2011.12.084
日期:2012.2
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.