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  1. 原著論文

Synthesis and preliminary evaluation of 18F-labeled 1-(6,7-dimethyl-4-(methylamino)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)-2-(trans-2-(6-fluoropyridin-3-yl)cyclopropyl)ethan-1-one for imaging muscarinic acetylcholine receptor subtype 4

https://repo.qst.go.jp/records/80110
https://repo.qst.go.jp/records/80110
e1d9a17c-88e0-42b0-beb1-0d10b46bf5d8
Item type 学術雑誌論文 / Journal Article(1)
公開日 2020-06-24
タイトル
タイトル Synthesis and preliminary evaluation of 18F-labeled 1-(6,7-dimethyl-4-(methylamino)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)-2-(trans-2-(6-fluoropyridin-3-yl)cyclopropyl)ethan-1-one for imaging muscarinic acetylcholine receptor subtype 4
言語
言語 eng
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
アクセス権
アクセス権 metadata only access
アクセス権URI http://purl.org/coar/access_right/c_14cb
著者 Deng, Xiaoyun

× Deng, Xiaoyun

WEKO 873840

Deng, Xiaoyun

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Zhang, Yiding

× Zhang, Yiding

WEKO 873841

Zhang, Yiding

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Rong, Jian

× Rong, Jian

WEKO 873842

Rong, Jian

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 873843

Kumata, Katsushi

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Shao, Tuo

× Shao, Tuo

WEKO 873844

Shao, Tuo

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Wang, Gangqiang

× Wang, Gangqiang

WEKO 873845

Wang, Gangqiang

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Hatori, Akiko

× Hatori, Akiko

WEKO 873846

Hatori, Akiko

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Mori, Wakana

× Mori, Wakana

WEKO 873847

Mori, Wakana

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Yu, Qingzhen

× Yu, Qingzhen

WEKO 873848

Yu, Qingzhen

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Kuan, Hu

× Kuan, Hu

WEKO 873849

Kuan, Hu

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 873850

Fujinaga, Masayuki

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Shao, Yihan

× Shao, Yihan

WEKO 873851

Shao, Yihan

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Josephson, Lee

× Josephson, Lee

WEKO 873852

Josephson, Lee

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Sun, Shaofa

× Sun, Shaofa

WEKO 873853

Sun, Shaofa

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 873854

Ming-Rong, Zhang

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Liang, Huan

× Liang, Huan

WEKO 873855

Liang, Huan

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Zhang, Yiding

× Zhang, Yiding

WEKO 873856

en Zhang, Yiding

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 873857

en Kumata, Katsushi

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Hatori, Akiko

× Hatori, Akiko

WEKO 873858

en Hatori, Akiko

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Mori, Wakana

× Mori, Wakana

WEKO 873859

en Mori, Wakana

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Kuan, Hu

× Kuan, Hu

WEKO 873860

en Kuan, Hu

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 873861

en Fujinaga, Masayuki

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 873862

en Ming-Rong, Zhang

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Liang, Huan

× Liang, Huan

WEKO 873863

en Liang, Huan

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抄録
内容記述タイプ Abstract
内容記述 Positive allosteric modulators of muscarinic acetylcholine receptor subtype 4 have been identified as promising activators for the treatment of neurological disorders and neurodegenerative diseases, including schizophrenia, Alzheimer's disease (AD) and dementia with Lewy bodies (DLB). Herein we report the synthesis and preliminary evaluation of a 18F-labeled positron emission tomography ligand based on a M4 activator (7). 18F-Isotopologue of 7 was prepared in a reasonable radiochemical yield with high radiochemical purity (>99%) and high molar activity (>37 GBq/µmol). In vitro autoradiography studies indicated that the ligand possessed moderate in vitro specific binding. Dynamic PET studies in vivo demonstrated that [18F]7 (also named as [18F]M4R-1911) failed to cross the blood–brain barrier. Therefore, further chemical scaffold optimization in chemotype of 7 is necessary to overcome limited brain permeability and improve specific binding.
書誌情報 Tetrahedron Letters

巻 61, 号 27, 発行日 2020-05
出版者
出版者 Elsevier
ISSN
収録物識別子タイプ ISSN
収録物識別子 0040-4039
DOI
識別子タイプ DOI
関連識別子 10.1016/j.tetlet.2020.152060
関連サイト
識別子タイプ URI
関連識別子 https://www.sciencedirect.com/science/article/pii/S0040403920305062
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