title: (E)-5-styryl-1H-indole and (E)-6-styrylquinoline derivatives serve as probes for β-amyloid plaques.
abstract: We report the synthesis and biological evaluation of novel (E)-5-styryl-1H-indole and (E)-6-styrylquinoline derivatives as probes for imaging β-amyloid (Aβ) plaques. These derivatives showed binding affinities for Aβ₁₋₄₀ aggregates with K(i) values varying from 4.1 to 288.4 nM. (E)-5-(4-iodostyryl)-1H-indole (8) clearly stained Aβ plaques in the brain sections of Alzheimer's disease (AD) model mice (APP/PS1). Furthermore, autoradiography for [¹²⁵I]8 displayed intense and specific labeling of Aβ plaques in the brain sections mentioned above with low background. In biodistribution experiments using normal mice [¹²⁵I]8 showed high initial brain uptake followed by rapid washout (4.27 and 0.64% ID/g at 2 and 30 min post injection, respectively). These findings suggests that [¹²³I]8 may be a potential SPECT imaging agent for detecting Aβ plaques in AD brain.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yang
authors.forename: Hong-Mei
authors.initials: HM
authors.lastname: Jia
authors.forename: Bo-Li
authors.initials: BL
authors.lastname: Liu
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000378:metabolism; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000473:pathology*; D005260:Female; D007211:Indoles / Q000737:chemistry / Q000378:metabolism; D007457:Iodine Radioisotopes / Q000378:metabolism; D051379:Mice; D008822:Mice, Transgenic; D015335:Molecular Probes / Q000737:chemistry / Q000378:metabolism; D058225:Plaque, Amyloid / Q000175:diagnosis* / Q000378:metabolism; D011485:Protein Binding; D011804:Quinolines / Q000737:chemistry / Q000378:metabolism; D011877:Radionuclide Imaging; D013194:Staining and Labeling
chemical_list: D016229:Amyloid beta-Peptides; D007211:Indoles; D007457:Iodine Radioisotopes; D015335:Molecular Probes; D011804:Quinolines; C481600:styrylquinoline