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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

× Chen, Zhen

WEKO 761477

Chen, Zhen

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Mori, Wakana

× Mori, Wakana

WEKO 761478

Mori, Wakana

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Deng, Xiaoyun

× Deng, Xiaoyun

WEKO 761479

Deng, Xiaoyun

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Cheng, Ran

× Cheng, Ran

WEKO 761480

Cheng, Ran

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Ogasawara, Daisuke

× Ogasawara, Daisuke

WEKO 761481

Ogasawara, Daisuke

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Zhang, Genwei

× Zhang, Genwei

WEKO 761482

Zhang, Genwei

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A. Schafroth, Michael

× A. Schafroth, Michael

WEKO 761483

A. Schafroth, Michael

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Dahl, Kenneth

× Dahl, Kenneth

WEKO 761484

Dahl, Kenneth

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Fu, Hualong

× Fu, Hualong

WEKO 761485

Fu, Hualong

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Hatori, Akiko

× Hatori, Akiko

WEKO 761486

Hatori, Akiko

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Shao, Tuo

× Shao, Tuo

WEKO 761487

Shao, Tuo

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Zhang, Yiding

× Zhang, Yiding

WEKO 761488

Zhang, Yiding

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Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 761489

Yamasaki, Tomoteru

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Zhang, Xiaofei

× Zhang, Xiaofei

WEKO 761490

Zhang, Xiaofei

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Rong, Jian

× Rong, Jian

WEKO 761491

Rong, Jian

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Yu, Qingzhen

× Yu, Qingzhen

WEKO 761492

Yu, Qingzhen

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Kuan, Hu

× Kuan, Hu

WEKO 761493

Kuan, Hu

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 761494

Fujinaga, Masayuki

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Xie, Lin

× Xie, Lin

WEKO 761495

Xie, Lin

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 761496

Kumata, Katsushi

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Gou, Yuancheng

× Gou, Yuancheng

WEKO 761497

Gou, Yuancheng

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Chen, Jingjin

× Chen, Jingjin

WEKO 761498

Chen, Jingjin

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Gu, Shuyin

× Gu, Shuyin

WEKO 761499

Gu, Shuyin

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Bao, Liang

× Bao, Liang

WEKO 761500

Bao, Liang

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Lu, Wang

× Lu, Wang

WEKO 761501

Lu, Wang

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Lee Collier, Thomas

× Lee Collier, Thomas

WEKO 761502

Lee Collier, Thomas

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Vasdev, Neil

× Vasdev, Neil

WEKO 761503

Vasdev, Neil

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Shao, Yihan

× Shao, Yihan

WEKO 761504

Shao, Yihan

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Jun-An, Ma

× Jun-An, Ma

WEKO 761505

Jun-An, Ma

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F. Cravatt, Benjamin

× F. Cravatt, Benjamin

WEKO 761506

F. Cravatt, Benjamin

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Fowler, Christopher

× Fowler, Christopher

WEKO 761507

Fowler, Christopher

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Josephson, Lee

× Josephson, Lee

WEKO 761508

Josephson, Lee

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 761509

Ming-Rong, Zhang

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Liang, Huan

× Liang, Huan

WEKO 761510

Liang, Huan

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Mori, Wakana

× Mori, Wakana

WEKO 761511

en Mori, Wakana

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Hatori, Akiko

× Hatori, Akiko

WEKO 761512

en Hatori, Akiko

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Zhang, Yiding

× Zhang, Yiding

WEKO 761513

en Zhang, Yiding

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Yamasaki, Tomoteru

× Yamasaki, Tomoteru

WEKO 761514

en Yamasaki, Tomoteru

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Kuan, Hu

× Kuan, Hu

WEKO 761515

en Kuan, Hu

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Fujinaga, Masayuki

× Fujinaga, Masayuki

WEKO 761516

en Fujinaga, Masayuki

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Xie, Lin

× Xie, Lin

WEKO 761517

en Xie, Lin

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Kumata, Katsushi

× Kumata, Katsushi

WEKO 761518

en Kumata, Katsushi

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Lu, Wang

× Lu, Wang

WEKO 761519

en Lu, Wang

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Ming-Rong, Zhang

× Ming-Rong, Zhang

WEKO 761520

en Ming-Rong, Zhang

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Liang, Huan

× Liang, Huan

WEKO 761521

en 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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