| Abstract
| - In vivo imaging of β-amyloid (Aβ) peptide aggregates in the brain may lead to early detectionof Alzheimer's disease (AD) and monitoring of the progression and effectiveness of AD treatment.The purpose of this study was to develop novel amyloid imaging agents based on flavone as acore structure. Radioiodinated flavone derivatives were designed and synthesized. The bindingaffinities of flavone derivatives for Aβ aggregates varied from 13 to 77 nM. When in vitro plaquelabeling was carried out using post-mortem AD brain sections, all flavones intensely stainednot only amyloid plaques but also cerebrovascular amyloids. In biodistribution studies usingnormal mice, they displayed high brain uptakes ranging from 3.2 to 4.1% ID/g at 2 minpostinjection. The radioactivity washed out from the brain rapidly (0.5−1.9% ID/g at 30 min),which is highly desirable for amyloid imaging agents. The results in the study suggest thatthese classes of radioiodinated flavones may be useful candidates as potential imaging agentsfor amyloid plaques.
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