title: Novel ¹⁸F-labeled dibenzylideneacetone derivatives as potential positron emission tomography probes for in vivo imaging of β-amyloid plaques.
abstract: A series of dibenzylideneacetones were synthesized and evaluated as imaging probes for β-amyloid plaques. They displayed high binding affinity to Aβ(1-42) aggregates (K(i) = 6.4 for 8, K(i) = 3.0 for 9), and the high binding were confirmed by in vitro autoradiography with AD human and transgenic mouse brain sections. Two of them were selected for (18)F-labeling directly on the benzene ring. In biodistribution experiments, [(18)F]8 and [(18)F]9 displayed high initial uptakes (9.29 ± 0.41 and 5.38 ± 0.68% ID/g) and rapid washouts from the normal brain (brain(2 min)/brain(60 min) ratios of 21.6 and 13.4). These preliminary results suggest that [(18)F]8 and [(18)F]9 may be used as potential PET imaging agents for the detection of Aβ plaques in the brain.
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors: Zijing
authors: Z
authors: Li
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China. Electronic address: cmc@bnu.edu.cn.
authors: Mengchao
authors: M
authors: Cui
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China; Department of Nuclear Medicine, Chinese PLA General Hospital, Beijing 100853, PR China. Electronic address: zhangjm301@163.com.
authors: Jinming
authors: J
authors: Zhang
authors: Wuhan Institute for Neuroscience and Neuroengineering, South-Central University for Nationalities, Wuhan 430074, PR China.
authors: Jiapei
authors: J
authors: Dai
authors: Department of Nuclear Medicine, Chinese PLA General Hospital, Beijing 100853, PR China.
authors: Xiaojun
authors: X
authors: Zhang
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors: Peng
authors: P
authors: Chen
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors: Hongmei
authors: H
authors: Jia
authors: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors: Boli
authors: B
authors: Liu
mesh_terms: D016229:Amyloid beta-Peptides / Q000032:analysis / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000378:metabolism / Q000473:pathology; D005456:Fluorescent Dyes / Q000138:chemical synthesis / Q000737:chemistry; D005462:Fluorine Radioisotopes; D006801:Humans; D051379:Mice; D008810:Mice, Inbred C57BL; D008822:Mice, Transgenic; D057054:Molecular Imaging; D015394:Molecular Structure; D010422:Pentanones / Q000138:chemical synthesis / Q000737:chemistry; D010446:Peptide Fragments / Q000032:analysis / Q000378:metabolism*; D049268:Positron-Emission Tomography; D013194:Staining and Labeling
chemical_list: D016229:Amyloid beta-Peptides; D005456:Fluorescent Dyes; D005462:Fluorine Radioisotopes; D010422:Pentanones; D010446:Peptide Fragments; C075222:amyloid beta-protein (1-42)
keywords: AD; Aβ plaques; Dibenzylideneacetone derivatives; PET imaging agents