期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 1, 期 7, 页码 321-325出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml100082x
关键词
Alzheimer's disease; fluorine-18; benzofuran; positron emission tomography (PET)
资金
- Program for Promotion of Fundamental Studies in Health Sciences of the National Institute of Biomedical Innovation (NIBIO)
- Ministry of Education, Culture, Sports, Science and Technology, Japan
A series of fluorinated benzofuran derivatives as potential tracers for positron emission tomography (PET) targeting beta-amyloid plaques in the brains of patients with Alzheimer's disease (AD) were synthesized and evaluated. The derivatives were produced using an intramolecular Wittig reaction. In experiments in vitro, all displayed high affinity for A beta(1-42) aggregates with K-i values in the nanomolar range. Radiofluorinated 17,[F-18]17, in particular labeled beta-amyloid plaques in sections of Tg2576 mouse brain and displayed high uptake (5.66% ID/g) at 10 min postinjection, sufficient for PET imaging. In addition, in vivo beta-amyloid plaque labeling can be clearly demonstrated with [F-18]17 in Tg2576 mice. In conclusion, [F-18]17 may be useful for detecting beta-amyloid plaques in patients with AD.
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