Push-pull benzothiazole derivatives as probes for detecting beta-amyloid plaques in Alzheimer's brains.
We synthesized push-pull benzothiazole derivatives and evaluated their potential as beta-amyloid imaging probes. In binding experiments in vitro, the benzothiazoles showed excellent affinity for synthetic Abeta(1-42) aggregates. beta-Amyloid plaques in the mouse and human brain were clearly visualized with the benzothiazoles, reflecting the results in vitro. These compounds may be a useful scaffold for the development of novel PET/SPECT and fluorescent tracers for detecting beta-amyloid in Alzheimer's brains.
Ono
Masahiro
M
Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Yoshida Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan. ono@pharm.kyoto-u.ac.jp
Hayashi
Shun
S
Kimura
Hiroyuki
H
Kawashima
Hidekazu
H
Nakayama
Morio
M
Saji
Hideo
H
D000544:Alzheimer Disease / Q000000981:diagnostic imaging*; D016229:Amyloid beta-Peptides / Q000032:analysis*; D000818:Animals; D052160:Benzothiazoles / Q000138:chemical synthesis*; D006801:Humans; D051379:Mice; D015336:Molecular Probe Techniques; D010446:Peptide Fragments / Q000032:analysis*; D049268:Positron-Emission Tomography; D015899:Tomography, Emission-Computed, Single-Photon
D016229:Amyloid beta-Peptides; D052160:Benzothiazoles; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42)