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Synthesis and characterization of novel phenylindoles as potential probes for imaging of beta-amyloid plaques in the brain.
http://hdl.handle.net/10069/23596
http://hdl.handle.net/10069/23596ec66780e-1ba5-480b-9b7a-7bf4abdcca33
名前 / ファイル | ライセンス | アクション |
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BMC18_4740.pdf (1.0 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 characterization of novel phenylindoles as potential probes for imaging of beta-amyloid plaques in the brain. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | β-amyloid | |||||
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 | Imaging | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Phenylindole | |||||
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× Haratake, Mamoru× Kobashi, Nobuya× Saji, Hideo× Nakayama, Morio |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | We synthesized a novel series of phenylindole (PI) derivatives and evaluated their biological activities as probes for imaging Abeta plaques in vivo. The affinity for Abeta plaques was assessed by an in vitro-binding assay using pre-formed synthetic Abeta aggregates. 2-Phenyl-1H-indole (2-PI) derivatives showed high affinity for Abeta42 aggregates with K(i) values ranging from 4 to 32nM. 2-PI derivatives clearly stained Abeta plaques in an animal model of AD. In biodistribution experiments using normal mice, 2-PI derivatives displayed sufficient uptake for imaging, ranging from 1.1% to 2.6% ID/g. Although additional modifications are necessary to improve uptake by and clearance from the brain, 2-PI derivatives may be useful as a backbone structure to develop novel Abeta imaging agents. | |||||
書誌情報 |
Bioorganic & medicinal chemistry 巻 18, 号 13, p. 4740-4746, 発行日 2010-05-13 |
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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 | 20605471 | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmc.2010.05.013 | |||||
権利 | ||||||
権利情報 | Copyright © 2010 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, 18(13), pp.4740-4746; 2010 |