A novel ¹⁸F-labelled high affinity agent for PET imaging of the translocator protein.

ABSTRACT: The translocator protein (TSPO) is an important target for imaging focal neuroinflammation in diseases such as brain cancer, stroke and neurodegeneration, but current tracers for non-invasive imaging of TSPO have important limitations. We present the synthesis and evaluation of a novel 3-fluoromethylquinoline-2-carboxamide, AB5186, which was prepared in eight steps using a one-pot two component indium(iii)-catalysed reaction for the rapid and efficient assembly of the 4-phenylquinoline core. Biological assessment and the implementation of a physicochemical study showed AB5186 to have low nanomolar affinity for TSPO, as well as optimal plasma protein binding and membrane permeability properties. Generation of [¹⁸F]-AB5186 through ¹⁸F incorporation was achieved in good

SUBMITTER: Blair A 

PROVIDER: S-EPMC5667507 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature