Al¹⁸F-NODA Benzothiazole Derivatives as Imaging Agents for Cerebrovascular Amyloid in Cerebral Amyloid Angiopathy.

ABSTRACT: In this study, we synthesized four novel Al^18/19F-labeled 2-phenylbenzothiazole derivatives conjugated to 1,4,7-triazacyclononane-1,4-diacetic acid via alkyl linkers and evaluated them as imaging agent targets to amyloid-β (Aβ) plaques deposited in the blood vessels of cerebral amyloid angiopathy (CAA) brain. The four ligands exhibited moderate-to-high binding ability to Aβ_1-42 aggregates, of which complex 17 possessing the most potent affinity (K _i = 11.3 nM) was selected for further biological evaluations. In vitro fluorescent staining and in vitro autoradiography studies on brain sections from CAA patients proved that this ligand could label Aβ deposits in blood vessels selectively. In biodistribution study, [¹⁸F]17 can ha

SUBMITTER: Song J 

PROVIDER: S-EPMC6217595 | biostudies-literature | 2018 Oct

REPOSITORIES: biostudies-literature