title: Molecular imaging of β-amyloid plaques with near-infrared boron dipyrromethane (BODIPY)-based fluorescent probes.
abstract: The formation of β-amyloid (Aβ) plaques is a critical neurodegenerative change in Alzheimer disease (AD). We designed and synthesized novel boron dipyrromethane (BODIPY)-based Aβ probes (BAPs) and evaluated their utility for near-infrared fluorescence imaging of Aβ plaques in the brain. In binding experiments in vitro, BAPs showed high affinity for synthetic Aβ aggregates (Kd  =  18-149 nM). Furthermore, BAPs clearly stained Aβ plaques in sections of Tg2576 mice. In mouse brain tissue, BAPs showed sufficient uptake for optical imaging. In addition, ex vivo fluorescent staining of brain sections from Tg2576 mice after the injection of BAP-2 showed selective binding of Aβ plaques with little nonspecific binding. BAPs may be useful as a near-infrared fluorescent probe for imaging Aβ plaques.
authors.affiliation: Department of Patho-Functional Bioanalysis, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto 606-8501, Japan.
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Watanabe
authors.forename: Masahiro
authors.initials: M
authors.lastname: Ono
authors.forename: Kenji
authors.initials: K
authors.lastname: Matsumura
authors.forename: Masashi
authors.initials: M
authors.lastname: Yoshimura
authors.forename: Hiroyuki
authors.initials: H
authors.lastname: Kimura
authors.forename: Hideo
authors.initials: H
authors.lastname: Saji
mesh_terms: D000818:Animals; D001896:Boron Compounds / Q000493:pharmacokinetics; D001921:Brain / Q000473:pathology; D005260:Female; D005453:Fluorescence; D005456:Fluorescent Dyes; D007700:Kinetics; D051379:Mice; D008822:Mice, Transgenic; D057054:Molecular Imaging / Q000379:methods*; D058225:Plaque, Amyloid / Q000175:diagnosis* / Q000473:pathology; D019265:Spectroscopy, Near-Infrared; D013194:Staining and Labeling; D014018:Tissue Distribution
chemical_list: C095489:4,4-difluoro-4-bora-3a,4a-diaza-s-indacene; D001896:Boron Compounds; D005456:Fluorescent Dyes