Radiofluorination of oxazole-carboxamides for preclinical PET neuroimaging of GSK-3

Journal of Fluorine Chemistry(2021)

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摘要
•Glycogen synthase kinase 3 (GSK-3) is an enzyme that is dysregulated in cancer and brain health illnesses.•No suitable fluorine-18 labeled GSK-3 radiotracer for positron emission tomography (PET) exists.•Two oxazole-4-carboxamides were labeled with [18F]fluoride.•Radiotracers were evaluated in rodents and in non-human primate showing good brain uptake.•[18F]OCM-49 and [18F]OCM-50 are promising tracers for imaging of GSK-3 in the brain.
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关键词
Glycogen synthase kinase 3,GSK-3,Fluorine-18,PET imaging,Copper-mediated radiofluorination,Neuroimaging
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