Positron emission tomography (PET) using 18F-labeled radiotracers is an important and rapidly progressing research area. These tracers have been widely used to study and visualize human disease pathology in a non-invasive and dynamic manner. Herein, we report the synthesis and tau- staining utility of [18F]T807, a 2-Fluoro-substituted pyridine azacarbazole that was prepared from a trialkylammonium-substituted pyridine salt. This radiolabeling precursor was obtained from the corresponding pyridine N-oxide. Binding studies of [18F]T807 to human brain-derived PHF-tau yielded an average Kd of 0.57 nM. The usefulness of [18F]T807 for detecting PHF-tau was further demonstrated by autoradiography on brain sections from patients that were afflicted with Alzheimer’s Disease (AD) and diverse non-AD tauopathies such as Pick’s disease and Progressive Supranuclear Palsy (PSP). A fluorescent probe, T557, was used as a surrogate of [18F]T807 to show by immunofluorescence that tau binding co-localized with tau-specific antibodies AT8, AT100, 3R-Tau and 4R-Tau in AD and non-AD samples of interest

18F-T807: A PET imaging compound for detecting tau in alzheimer’s and non-alzheimer’s neurodegenerative diseases

249th National Meeting (2015)

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