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Development of alkoxy styrylchromone derivatives for imaging of cerebral amyloid-β plaques with SPECT
http://hdl.handle.net/10069/35661
http://hdl.handle.net/10069/3566188478238-f24b-46e5-a35a-ddd862716f14
名前 / ファイル | ライセンス | アクション |
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Supple.pdf (149.1 kB)
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BMCL25_22738.pdf (299.7 kB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2017-08-16 | |||||
タイトル | ||||||
タイトル | Development of alkoxy styrylchromone derivatives for imaging of cerebral amyloid-β plaques with SPECT | |||||
言語 | ||||||
言語 | eng | |||||
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 | Amyloid-β plaque | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Single photon emission computed tomography (SPECT) | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | Styrylchromone | |||||
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 |
Fuchigami, Takeshi
× Fuchigami, Takeshi× Ogawa, Ayaka× Yamashita, Yuki× Haratake, Mamoru× Watanabe, Hiroyuki× Ono, Masahiro× Kawasaki, Masao× Yoshida, Sakura× Nakayama, Morio |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Abstract We report here the development of radioiodinated styrylchromone derivatives with alkoxy groups as single photon emission computed tomography (SPECT) imaging probes for cerebral amyloid-β (Aβ) plaques. Among the derivatives, the methoxy derivative 14 and the dimethoxy derivative 15 displayed relatively high affinity for the Aβ(1-42) aggregates with Ki values of 22 and 46 nM, respectively. Fluorescent imaging demonstrated that 14 and 15 clearly labeled thioflavin-S positive Aβ plaques in the brain sections of Tg2576 transgenic mice. In the in vivo studies, [125I]14 and [125I]15 showed high initial brain uptake expressed as the percentage of the injected dose per gram (2.25% and 2.49% ID/g at 2 min, respectively) with favorable clearance (0.12% and 0.20% ID/g at 180 min, respectively) from the brain tissue of normal mice. Furthermore, in vitro autoradiography confirmed that [125I]15 binds thioflavin-S positive regions in Tg2576 mouse brain sections. The derivative 15 may be a potential scaffold for the development of in vivo imaging probes targeting Aβ plaques in the brain. In particular, further structural modifications are required to improve the compounds binding affinity for Aβ. | |||||
書誌情報 |
Bioorganic & Medicinal Chemistry Letters 巻 25, 号 16, p. 3363-3367, 発行日 2015-08-15 |
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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 | 0960894X | |||||
DOI | ||||||
関連タイプ | isVersionOf | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.bmcl.2015.05.048 | |||||
権利 | ||||||
権利情報 | c 2015 Elsevier Ltd. Licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International http://creativecommons.org/licenses/by-nc-nd/4.0/ | |||||
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 Letters, 25(16), pp.3363-3367; 2015 |