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Matsumura, Ono, Yoshimura, Kimura, Watanabe, Okamoto, Ihara, Takahashi, Saji (2013) Synthesis and biological evaluation of novel styryl benzimidazole derivatives as probes for imaging of neurofibrillary tangles in Alzheimer's disease Bioorganic & medicinal chemistry 21(11) 3356-62


This paper describes the synthesis and biological evaluation of styrylbenzimidazole (SBIM) derivatives as agents for imaging neurofibrillary tangles (NFT) in patients with Alzheimer's disease (AD). SBIM derivatives were prepared with 4-iodobenzene-1,2-diamine and substituted cinnamaldehydes. In binding experiments using recombinant tau and Aβ(1-42) aggregates, SBIM-3 showed higher affinity for the tau aggregates than Aβ(1-42) aggregates (ratio of K(d) values was 2.73). In in vitro autoradiography and fluorescent staining, [(125)I]SBIM-3 (or SBIM-3) bound NFT in sections of AD brain tissue. In biodistribution experiments using normal mice, all [(125)I]SBIM derivatives showed high initial uptake into (3.20-4.11%ID/g at 2 min after the injection) and rapid clearance from (0.12-0.33%ID/g at 60 min after the injection) the brain. In conclusion, appropriate structural modifications of SBIM derivatives could lead to more useful agents for the in vivo imaging of NFT in AD brains.


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