Journal
CHEMBIOCHEM
Volume 8, Issue 14, Pages 1679-1687Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/cbic.200700154
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Funding
- NCRR NIH HHS [C06 RR-16572] Funding Source: Medline
- NIA NIH HHS [AG15408, AG20245] Funding Source: Medline
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A group of styryl-based neutral compounds has been synthesized in this study for potential use as in vivo imaging agents for beta-amyloid plaques. Of 56 candidates, 14 compounds were found to label beta-amyloid plaques well on Alzheimer's disease (AD) human brain sections in vitro. The binding affinity to beta-amyloid fibrils was then determined by measuring the change in fluorescence intensity. Interestingly, we found that a class of quinaldine-styryl scaffold compounds displays specific binding to beta-amyloid fibrils. A representative compound, STB-8, was used in ex vivo and in vivo imaging experiments on an AD transgenic mouse model and demonstrated excellent blood-brain barrier (BBB) permeability and specific staining of the AD beta-amyloid plaques.
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