Structure-Activity and Brain Kinetics Relationships of ¹⁸F-Labeled Benzimidazopyridine Derivatives as Tau PET Tracers.

ABSTRACT: Noninvasive imaging of tau aggregates with a positron emission tomography (PET) tracer is useful for the diagnosis and staging of Alzheimer's disease (AD). Recently, we found that benzimidazopyridine (BIP) is an attractive scaffold for developing PET and single photon computed emission tomography tracers targeting tau aggregates. In this study, we designed and synthesized five novel ¹⁸F-labeled compounds with various substituted groups or atoms at the 7-position of the BIP scaffold. In in vitro autoradiographic studies, all ¹⁸F-labeled BIP derivatives selectively bound to tau aggregates deposited in AD brain sections. On the other hand, the initial brain uptake of these compounds was affected by the type of substituted group or halogen atom introduced into the

SUBMITTER: Watanabe H 

PROVIDER: S-EPMC7883465 | biostudies-literature | 2021 Feb

REPOSITORIES: biostudies-literature