Full metadata record
DC Field | Value | Language |
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dc.contributor.author | 김범산 | * |
dc.date.accessioned | 2016-08-28T12:08:37Z | - |
dc.date.available | 2016-08-28T12:08:37Z | - |
dc.date.issued | 2011 | * |
dc.identifier.issn | 0968-0896 | * |
dc.identifier.other | OAK-7552 | * |
dc.identifier.uri | https://dspace.ewha.ac.kr/handle/2015.oak/221602 | - |
dc.description.abstract | To develop agents for radionuclide imaging Aβ plaques in vivo, we prepared three fluorine-substituted analogs of arylbenzothiazole class; compound 2 has a high affinity for Aβ (Ki = 5.5 nM) and the specific binding to Aβ in fluorescent staining. In preparation for the synthesis of these arylbenzothiazole analogs in radiolabeled form as an Aβ plaques-specific positron emission tomography (PET) imaging probe, we investigated synthetic route suitable for its labeling with the short-lived PET radionuclide fluorine-18 (t1/2 = 110 min) and diaryliodonium tosylate precursors (12, 13a-e and 14). 2-Aryl-6-[18F]fluorobenzothiazoles ([18F]1-3) were synthesized in efficiently short reaction times (40-60 min) with high radiochemical yields (19-40%), purities (>95%) and specific activities (85-118 GBq/μmol). Tissue distribution studies showed that high radioactivity of [18F]2 accumulated in the brain with rapid clearance in healthy mice. Radioactive metabolites were analyzed in brain samples of mice and corresponded to 81% of parent remained by 30 min after a tail-vein injection. These results suggest that [18F]2 is a promising probe for evaluation of Aβ plaques imaging in brain using PET. © 2011 Elsevier Ltd. All rights reserved. | * |
dc.language | English | * |
dc.title | Aromatic radiofluorination and biological evaluation of 2-aryl-6-[ 18F]fluorobenzothiazoles as a potential positron emission tomography imaging probe for β-amyloid plaques | * |
dc.type | Article | * |
dc.relation.issue | 9 | * |
dc.relation.volume | 19 | * |
dc.relation.index | SCI | * |
dc.relation.index | SCIE | * |
dc.relation.index | SCOPUS | * |
dc.relation.startpage | 2980 | * |
dc.relation.lastpage | 2990 | * |
dc.relation.journaltitle | Bioorganic and Medicinal Chemistry | * |
dc.identifier.doi | 10.1016/j.bmc.2011.03.029 | * |
dc.identifier.wosid | WOS:000289834600022 | * |
dc.identifier.scopusid | 2-s2.0-79955471678 | * |
dc.author.google | Lee B.C. | * |
dc.author.google | Kim J.S. | * |
dc.author.google | Kim B.S. | * |
dc.author.google | Son J.Y. | * |
dc.author.google | Hong S.K. | * |
dc.author.google | Park H.S. | * |
dc.author.google | Moon B.S. | * |
dc.author.google | Jung J.H. | * |
dc.author.google | Jeong J.M. | * |
dc.author.google | Kim S.E. | * |
dc.contributor.scopusid | 김범산(35223582600) | * |
dc.date.modifydate | 20240123125716 | * |