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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
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Chen, Zhen (author)
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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, Christopher (author)
- Umeå universitet,Farmakologi
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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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(creator_code:org_t)
- 2019-03-04
- 2019
- English.
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In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 62:7, s. 3336-3353
- Related links:
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https://europepmc.or...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Subject headings
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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.
Subject headings
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinsk bioteknologi -- Medicinsk bioteknologi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Medical Biotechnology -- Medical Biotechnology (hsv//eng)
Publication and Content Type
- ref (subject category)
- art (subject category)
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To the university's database
- 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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show more...
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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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show less...
- About the subject
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- MEDICAL AND HEALTH SCIENCES
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MEDICAL AND HEAL ...
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and Medical Biotechn ...
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and Medical Biotechn ...
- Articles in the publication
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Journal of Medic ...
- By the university
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Umeå University