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Design, Synthesis, ...
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
- Article/chapterEnglish2019
Publisher, publication year, extent ...
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2019-03-04
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American Chemical Society (ACS),2019
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printrdacarrier
Numbers
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LIBRIS-ID:oai:DiVA.org:umu-158574
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https://urn.kb.se/resolve?urn=urn:nbn:se:umu:diva-158574URI
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https://doi.org/10.1021/acs.jmedchem.8b01778DOI
Supplementary language notes
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Language:English
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Summary in:English
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Classification
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Subject category:ref swepub-contenttype
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Subject category:art swepub-publicationtype
Notes
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Monoacylglycerol lipase (MAGL) is a senile 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 C-11 or F-18. [C-11]8 ([C-11]MAGL-2-11) exhibited high brain uptake and excellent binding specificity in the brain toward MAGL. Reversible radioligands [C-11]17 ([C-11]PAD) and [F-18]37 ([F-18]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.
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Mori, Wakana
(author)
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Deng, Xiaoyun
(author)
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Cheng, Ran
(author)
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Ogasawara, Daisuke
(author)
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Zhang, Genwei
(author)
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Schafroth, Michael A.
(author)
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Dahl, Kenneth
(author)
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Fu, Hualong
(author)
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Hatori, Akiko
(author)
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Shao, Tuo
(author)
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Zhang, Yiding
(author)
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Yamasaki, Tomoteru
(author)
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Zhang, Xiaofei
(author)
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Rong, Jian
(author)
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Yu, Qngzhen
(author)
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Hu, Kuan
(author)
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Fujinaga, Masayuki
(author)
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Xie, Lin
(author)
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Kumata, Katsushi
(author)
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Gou, Yuancheng
(author)
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Chen, Jingjin
(author)
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Gu, Shuyin
(author)
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Bao, Liang
(author)
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Wang, Lu
(author)
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Collier, Thomas Lee
(author)
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Vasdev, Neil
(author)
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Shao, Yihan
(author)
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Ma, Jun-An
(author)
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Cravatt, Benjamin F.
(author)
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Fowler, ChristopherUmeå universitet,Farmakologi(Swepub:umu)chfo0001
(author)
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Josephson, Lee
(author)
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Zhang, Ming-Rong
(author)
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Liang, Steven H.
(author)
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Umeå universitetFarmakologi
(creator_code:org_t)
Related titles
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In:Journal of Medicinal Chemistry: American Chemical Society (ACS)62:7, s. 3336-33530022-26231520-4804
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- By the author/editor
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Chen, Zhen
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Mori, Wakana
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Deng, Xiaoyun
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Cheng, Ran
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Ogasawara, Daisu ...
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Zhang, Genwei
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Schafroth, Micha ...
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Dahl, Kenneth
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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, Tomote ...
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Zhang, Xiaofei
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Rong, Jian
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Yu, Qngzhen
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Hu, Kuan
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Fujinaga, Masayu ...
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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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Wang, Lu
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Collier, Thomas ...
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Vasdev, Neil
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Shao, Yihan
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Ma, Jun-An
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Cravatt, Benjami ...
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Fowler, Christop ...
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Josephson, Lee
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Zhang, Ming-Rong
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Liang, Steven H.
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- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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Journal of Medic ...
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Umeå University