A series of dibenzylideneacetones were synthesized and evaluated as imaging probes for β-amyloid plaques. They displayed high binding affinity to Aβ(1-42) aggregates (K(i) = 6.4 for 8, K(i) = 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 (18)F-labeling directly on the benzene ring. In biodistribution experiments, [(18)F]8 and [(18)F]9 displayed high initial uptakes (9.29 ± 0.41 and 5.38 ± 0.68% ID/g) and rapid washouts from the normal brain (brain(2 min)/brain(60 min) ratios of 21.6 and 13.4). These preliminary results suggest that [(18)F]8 and [(18)F]9 may be used as potential PET imaging agents for the detection of Aβ plaques in the brain.
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