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Synthesis and biological evaluation of radioiodinated 2,5-diphenyl-1,3,4-oxadiazoles for detecting beta-amyloid plaques in the brain.
http://hdl.handle.net/10069/23595
http://hdl.handle.net/10069/235953fd395bf-cd9b-423e-99a9-56dc7094d949
名前 / ファイル | ライセンス | アクション |
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BMC17_6402.pdf (1.2 MB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2010-08-23 | |||||
タイトル | ||||||
タイトル | Synthesis and biological evaluation of radioiodinated 2,5-diphenyl-1,3,4-oxadiazoles for detecting beta-amyloid plaques in the brain. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | β-Amyloid plaques | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Alzheimer's disease | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | SPECT imaging | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
Watanabe, Hiroyuki
× Watanabe, Hiroyuki× Ono, Masahiro× Ikeoka, Ryoichi× Haratake, Mamoru× Saji, Hideo× Nakayama, Morio |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | This paper describes the synthesis and biological evaluation of a new series of 2,5-diphenyl-1,3,4-oxadiazole (1,3,4-DPOD) derivatives for detecting beta-amyloid plaques in Alzheimer's brains. The affinity for beta-amyloid plaques was assessed by an in vitro binding assay using pre-formed synthetic Abeta42 aggregates. The new series of 1,3,4-DPOD derivatives showed affinity for Abeta42 aggregates with K(i) values ranging from 20 to 349 nM. The 1,3,4-DPOD derivatives clearly stained beta-amyloid plaques in an animal model of Alzheimer's disease, reflecting the affinity for Abeta42 aggregates in vitro. Compared to 3,5-diphenyl-1,2,4-oxadiazole (1,2,4-DPOD) derivatives, they displayed good penetration of and fast washout from the brain in biodistribution experiments using normal mice. The novel radioiodinated 1,3,4-DPOD derivatives may be useful probes for detecting beta-amyloid plaques in the Alzheimer's brain. | |||||
書誌情報 |
Bioorganic & medicinal chemistry 巻 17, 号 17, p. 6402-6406, 発行日 2009-09-01 |
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出版者 | ||||||
出版者 | Elsevier Ltd. | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 09680896 | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 14643391 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA10938083 | |||||
PubMed番号 | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | PMID | |||||
関連識別子 | 19651517 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmc.2009.07.020 | |||||
権利 | ||||||
権利情報 | Copyright © 2009 Elsevier Ltd All rights reserved. | |||||
著者版フラグ | ||||||
出版タイプ | AM | |||||
出版タイプResource | http://purl.org/coar/version/c_ab4af688f83e57aa | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Bioorganic & medicinal chemistry, 17(17), pp.6402-6406; 2009 |