⁶⁸Ga-Labeled Benzothiazole Derivatives for Imaging Aβ Plaques in Cerebral Amyloid Angiopathy.

ABSTRACT: Timely diagnostic imaging plays a crucial role in managing cerebral amyloid angiopathy (CAA)-the condition in which amyloid β is deposited on blood vessels. To selectively map these amyloid plaques, we have designed amyloid-targeting ligands that can effectively complex with ⁶⁸Ga³⁺ while maintaining good affinity for amyloid β. In this study, we introduced novel 1,4,7-triazacyclononane-based bifunctional chelators (BFCs) that incorporate a benzothiazole moiety as the Aβ-binding fragment and form charged and neutral species with ⁶⁸Ga³⁺. In vitro autoradiography using 5xFAD and WT mouse brain sections (11-month-old) suggested strong and specific binding of the ⁶⁸Ga complexes to amyloid β. Biodistribution studies in CD-1 mice revealed a l

SUBMITTER: Huynh TT 

PROVIDER: S-EPMC9202065 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature