期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 21, 期 11, 页码 3356-3362出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.02.054
关键词
Alzheimer's disease; Neurofibrillary tangles; Tau; Imaging; Styryl benzimidazole
资金
- Funding Program for Next Generation World-Leading Researchers
- JSPS Research Fellowships for Young Scientists
- Grants-in-Aid for Scientific Research [24659564] Funding Source: KAKEN
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 A beta(1-42) aggregates, SBIM-3 showed higher affinity for the tau aggregates than Ab1-42 aggregates (ratio of K-d values was 2.73). In in vitro autoradiography and fluorescent staining, [I-125]SBIM-3 (or SBIM-3) bound NFT in sections of AD brain tissue. In biodistribution experiments using normal mice, all [I-125]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. (C) 2013 Elsevier Ltd. All rights reserved.
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