title: Fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes targeting amyloid-beta plaques in Alzheimer's disease.
abstract: Amyloid plaques, which are primarily composed of aggregated amyloid-beta (Aβ) peptide, are the neuropathological hallmarks of Alzheimer's disease (AD). Fluorescent markers containing 2-styrylpyridazin-3(2H)-ones were developed to detect intracellular aggregated Aβ peptides. Nine compounds exhibited a greater than 10-fold increase of in emission spectra before and after mixing with Aβ aggregates compared with before mixing. Among these compounds, compound 9n exhibited the highest affinity for Aβ aggregates (K(d)=1.84 μM) and selectively stained both aggregated intracellular Aβ and Aβ plaques in the transgenic AD model mice (APP/PS1). These preliminary results indicate that 2-styrylpyridazin-3(2H)-one derivatives are promising alternative fluorescence imaging agent for the study of AD.
authors.affiliation: Advanced Radiation Technology Institute, Korea Atomic Energy Research Institute, Jeongup 580-185, Republic of Korea.
authors.forename: Yong Dae
authors.initials: YD
authors.lastname: Park
authors.forename: Jeong Hoon
authors.initials: JH
authors.lastname: Park
authors.forename: Min Goo
authors.initials: MG
authors.lastname: Hur
authors.forename: Sang Wook
authors.initials: SW
authors.lastname: Kim
authors.forename: Jung-Joon
authors.initials: JJ
authors.lastname: Min
authors.forename: Seung-Hwan
authors.initials: SH
authors.lastname: Park
authors.forename: Yung Joon
authors.initials: YJ
authors.lastname: Yoo
authors.forename: Yong-Jin
authors.initials: YJ
authors.lastname: Yoon
authors.forename: Seung Dae
authors.initials: SD
authors.lastname: Yang
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000473:pathology; D016229:Amyloid beta-Peptides / Q000032:analysis*; D000818:Animals; D001921:Brain / Q000473:pathology; D004195:Disease Models, Animal; D005453:Fluorescence; D005456:Fluorescent Dyes / Q000737:chemistry; D006801:Humans; D051379:Mice; D008822:Mice, Transgenic; D058225:Plaque, Amyloid / Q000737:chemistry*; D011724:Pyridazines / Q000737:chemistry; D012680:Sensitivity and Specificity; D013050:Spectrometry, Fluorescence; D013194:Staining and Labeling / Q000379:methods
chemical_list: D016229:Amyloid beta-Peptides; D005456:Fluorescent Dyes; D011724:Pyridazines