title: Novel (E)-5-styryl-2,2'-bithiophene derivatives as ligands for β-amyloid plaques.
abstract: In continuation of our investigation on the bithiophene structure as potential β-amyloid probes, a series of (E)-5-styryl-2,2'-bithiophene (SBTP) derivatives was designed and synthesized. In vitro binding showed that all of them displayed high binding affinities to Aβ(1-42) aggregates (K(i)=0.10-41.05nM). Moreover, two radio-iodinated probes, [(125)I]-(E)-5-(4-iodostyryl)-2,2'-bithiophene ([(125)I]8) and [(125)I]-(E)-5-iodo-5'-(4-methoxystyryl)-2,2'-bithiophene ([(125)I]31) were prepared. Both of them displayed specific labeling of Aβ plaques in the brain sections of AD model mice with low background. In vivo biodistribution in normal mice indicated that [(125)I]8 exhibited high initial brain uptake (2.11% ID/g at 2 min) and rapid clearance (0.41% ID/g at 30 min). These preliminary results suggest that SBTP derivatives may be served as novel β-amyloid imaging probes.
authors.affiliation: Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Xinjiekouwai Street 19#, Beijing 100875, PR China.
authors.forename: Mengchao
authors.initials: M
authors.lastname: Cui
authors.forename: Zijing
authors.initials: Z
authors.lastname: Li
authors.forename: Ruikun
authors.initials: R
authors.lastname: Tang
authors.forename: Hongmei
authors.initials: H
authors.lastname: Jia
authors.forename: Boli
authors.initials: B
authors.lastname: Liu
mesh_terms: D000544:Alzheimer Disease / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D016229:Amyloid beta-Peptides / Q000737:chemistry*; D000818:Animals; D001692:Biological Transport; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D003287:Contrast Media / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D004195:Disease Models, Animal; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D008024:Ligands; D051379:Mice; D008822:Mice, Transgenic; D010446:Peptide Fragments / Q000737:chemistry*; D058225:Plaque, Amyloid / Q000175:diagnosis* / Q000000981:diagnostic imaging / Q000378:metabolism / Q000473:pathology; D049268:Positron-Emission Tomography; D011485:Protein Binding; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D013876:Thiophenes / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D016229:Amyloid beta-Peptides; D003287:Contrast Media; D007457:Iodine Radioisotopes; D008024:Ligands; D010446:Peptide Fragments; D019275:Radiopharmaceuticals; D013876:Thiophenes; C075222:amyloid beta-protein (1-42)