Neuropathological hallmarks of Alzheimer's disease are protein deposits consisting of senile plaques (SPs) and neurofibrillary tangles (NFTs).  In search of a reliable biomarker for this neurodegenerative disease, several PET imaging agents are currently being developed to detect �-amyloid in human AD brains, but there have been limited reports on such biomarkers targeting tau protein aggregates.  In our search of a [18F]-PET tracer suitable for AD imaging, we developed a competitive autoradiography screening method utilizing human AD brain sections and discovered several novel, heterocyclic tau binding agents that showed not only strong binding affinity to native tau tangles, but also almost no binding to �-amyloid.  Three lead compounds were further developed and in vitro and in vivo results indicate that these tracers show suitable properties and great promise as tau PET imaging agents.

Development of novel, selective [F18]-PET agents for imaging of tau in Alzheimer's brains

242nd National Meeting (2011)

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