Styryl-based compounds as potential in vivo imaging agents for beta-amyloid plaques.
Li Q,
Min J,
Ahn YH,
Namm J,
Kim EM,
Lui R,
Kim HY,
Ji Y,
Wu H,
Wisniewski T,
Chang YT.
Department of Chemistry, New York University, School of Medicine, New York, NY 11219, USA.
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.
PMID: 17705341 [PubMed - indexed for MEDLINE]