title: (99m)Tc-labeled-2-arylbenzoxazole derivatives as potential Aβ imaging probes for single-photon emission computed tomography.
abstract: Four neutral (99m)Tc/Re-labeled 2-arylbenzoxazole derivatives conjugated to bis (aminoethanethiol) (BAT) chelating ligand via a short propoxy spacer were synthesized and evaluated. In vitro binding assay showed that they displayed binding affinities to Aβ1-42 aggregates (Ki = 15.86-393.18 nM). In vitro autoradiography studies further confirmed the high and specific binding of [(99m)Tc]20 to β-amyloid plaques on brain sections of transgenic mice. Biodistribution study of [(99m)Tc]17-20 in normal mice displayed moderate initial brain uptake (0.96-1.55%ID/g at 2 min), and fast washed out from the brain (0.14-0.40%ID/g at 60 min), especially for [(99m)Tc]20 with a brain2min/brain60min ratio of 8.86. Taken together, these preliminary data suggested that [(99m)Tc]20 may be a potential imaging probe for detecting amyloid plaques in the brain.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors.forename: Xuedan
authors.initials: X
authors.lastname: Wang
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China. Electronic address: cmc@bnu.edu.cn.
authors.forename: Mengchao
authors.initials: M
authors.lastname: Cui
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors.forename: Jianhua
authors.initials: J
authors.lastname: Jia
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, PR China.
authors.forename: Boli
authors.initials: B
authors.lastname: Liu
mesh_terms: D000544:Alzheimer Disease / Q000000981:diagnostic imaging / Q000378:metabolism; D016229:Amyloid beta-Peptides / Q000378:metabolism*; D000818:Animals; D001583:Benzoxazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D005260:Female; D006801:Humans; D008024:Ligands; D008297:Male; D008810:Mice, Inbred C57BL; D008822:Mice, Transgenic; D015394:Molecular Structure; D010446:Peptide Fragments / Q000378:metabolism*; D058225:Plaque, Amyloid / Q000000981:diagnostic imaging / Q000378:metabolism; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics; D013667:Technetium / Q000737:chemistry*; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon / Q000379:methods*
chemical_list: D016229:Amyloid beta-Peptides; D001583:Benzoxazoles; D008024:Ligands; D010446:Peptide Fragments; D019275:Radiopharmaceuticals; C075222:amyloid beta-protein (1-42); D013667:Technetium
keywords: 2-Arylbenzoxazole; AD; SPECT; β-amyloid plaques