Novel 18F-labeled dibenzylideneacetone derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques

•Two dibenzylideneacetones derivatives were labeled with 18F on the benzene ring.•High affinity to Aβ1–42 aggregates was confirmed by binding assay & autoradiography.•[18F]8/9 displayed high initial uptakes and rapid washouts from the normal brain.

A series of dibenzylideneacetones were synthesized and evaluated as imaging probes for β-amyloid plaques. They displayed high binding affinity to Aβ1–42 aggregates (Ki = 6.4 for 8, Ki = 3.0 for 9), and the high binding were confirmed by in vitro autoradiography with AD human and transgenic mouse brain sections. Two of them were selected for 18F-labeling directly on the benzene ring. In biodistribution experiments, [18F]8 and [18F]9 displayed high initial uptakes (9.29 ± 0.41 and 5.38 ± 0.68% ID/g) and rapid washouts from the normal brain (brain2 min/brain60 min ratios of 21.6 and 13.4). These preliminary results suggest that [18F]8 and [18F]9 may be used as potential PET imaging agents for the detection of Aβ plaques in the brain.

Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide