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Styryl‐Based Compounds as Potential in vivo Imaging Agents for β‐Amyloid Plaques
Author(s) -
Li Qian,
Min Jaeki,
Ahn YoungHoon,
Namm Joshua,
Kim Eun Min,
Lui Rowena,
Kim Hye Yun,
Ji Yong,
Wu Hueizhi,
Wisniewski Thomas,
Chang YoungTae
Publication year - 2007
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700154
Subject(s) - in vivo , ex vivo , chemistry , amyloid (mycology) , biophysics , fibril , genetically modified mouse , in vitro , blood–brain barrier , preclinical imaging , biochemistry , transgene , biology , neuroscience , central nervous system , inorganic chemistry , microbiology and biotechnology , gene
A group of styryl‐based neutral compounds has been synthesized in this study for potential use as in vivo imaging agents for β‐amyloid plaques. Of 56 candidates, 14 compounds were found to label β‐amyloid plaques well on Alzheimer's disease (AD) human brain sections in vitro. The binding affinity to β‐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 β‐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 β‐amyloid plaques.