Styryl-Based Compounds as Potential in vivo Imaging Agents for beta-Amyloid Plaques.
Chembiochem : a European journal of chemical biology 2007 Aug 20; 8(14):1679-87
Li Q Q, Min J J, Ahn Y YH, Namm J J, Kim E EM, Lui R R, Kim H HY, Ji Y Y, Wu H H, Wisniewski T T, Chang Y YT
Department of Chemistry, New York University, New York, NY 11219, USA, Fax: (+1) 212-260-7905.
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.