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  1. 原著論文

Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton

https://repo.qst.go.jp/records/75641
https://repo.qst.go.jp/records/75641
25b4719e-ca97-4d3d-b3f3-585c77014f5c
Item type 学術雑誌論文 / Journal Article(1)
公開日 2019-04-18
タイトル
タイトル Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton
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 Chen, Zhen

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Mori, Wakana

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Deng, Xiaoyun

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Cheng, Ran

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Cheng, Ran

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Ogasawara, Daisuke

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Ogasawara, Daisuke

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Zhang, Genwei

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Zhang, Genwei

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A. Schafroth, Michael

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A. Schafroth, Michael

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Dahl, Kenneth

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Dahl, Kenneth

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Fu, Hualong

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Fu, Hualong

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Hatori, Akiko

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Shao, Tuo

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Zhang, Yiding

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Yamasaki, Tomoteru

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Zhang, Xiaofei

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Rong, Jian

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Yu, Qingzhen

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Kuan, Hu

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Fujinaga, Masayuki

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Xie, Lin

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Kumata, Katsushi

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Gou, Yuancheng

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Chen, Jingjin

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Gu, Shuyin

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Bao, Liang

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Lu, Wang

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Lee Collier, Thomas

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Vasdev, Neil

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Shao, Yihan

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Jun-An, Ma

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F. Cravatt, Benjamin

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Fowler, Christopher

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Josephson, Lee

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Ming-Rong, Zhang

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Liang, Huan

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Mori, Wakana

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Hatori, Akiko

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Zhang, Yiding

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Yamasaki, Tomoteru

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Kuan, Hu

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Fujinaga, Masayuki

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Xie, Lin

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Kumata, Katsushi

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Lu, Wang

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Ming-Rong, Zhang

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Liang, Huan

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抄録
内容記述タイプ Abstract
内容記述 Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological conditions, including chronic pain, inflammation, cancer, and neurodegeneration. Herein, we disclose a novel array of reversible and irreversible MAGL inhibitors by means of “tail switching” on a piperazinyl azetidine scaffold. We developed a lead irreversible-binding MAGL inhibitor 8 and reversible-binding compounds 17 and 37, which are amenable for radiolabeling with 11C or18F. [11C]8 ([11C]MAGL-2-11) exhibited high brain uptake and excellent binding specificity in the brain toward MAGL. Reversible radioligands [11C]17 ([11C]PAD) and [18F]37 ([18F]MAGL-4-11) also demonstrated excellent in vivo binding specificity toward MAGL in peripheral organs. This work may pave the way for the development of MAGL-targeted positron emission tomography tracers with tunability in reversible and irreversible binding mechanisms.
書誌情報 Journal of Medicinal Chemistry

巻 62, 号 7, p. 3336-3353, 発行日 2019-03
出版者
出版者 ACS Publications
ISSN
収録物識別子タイプ ISSN
収録物識別子 0022-2623
DOI
識別子タイプ DOI
関連識別子 10.1021/acs.jmedchem.8b01778
関連サイト
識別子タイプ URI
関連識別子 https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01719
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