WFRF:(Chen Kuan Yu)
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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
- Chen, Zhen (author)
- Mori, Wakana (author)
- Deng, Xiaoyun (author)
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- Cheng, Ran (author)
- Ogasawara, Daisuke (author)
- Zhang, Genwei (author)
- Schafroth, Michael A. (author)
- Dahl, Kenneth (author)
- Fu, Hualong (author)
- Hatori, Akiko (author)
- Shao, Tuo (author)
- Zhang, Yiding (author)
- Yamasaki, Tomoteru (author)
- Zhang, Xiaofei (author)
- Rong, Jian (author)
- Yu, Qngzhen (author)
- Hu, Kuan (author)
- Fujinaga, Masayuki (author)
- Xie, Lin (author)
- Kumata, Katsushi (author)
- Gou, Yuancheng (author)
- Chen, Jingjin (author)
- Gu, Shuyin (author)
- Bao, Liang (author)
- Wang, Lu (author)
- Collier, Thomas Lee (author)
- Vasdev, Neil (author)
- Shao, Yihan (author)
- Ma, Jun-An (author)
- Cravatt, Benjamin F. (author)
- Josephson, Lee (author)
- Zhang, Ming-Rong (author)
- Liang, Steven H. (author)
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- (creator_code:org_t)
- 2019-03-04
- 2019
- English.
- In: Journal of Medicinal Chemistry. - : American Chemical Society (ACS). - 0022-2623 .- 1520-4804. ; 62:7, s. 3336-3353
- Journal article (peer-reviewed)
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)
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- Chen, Zhen
- Mori, Wakana
- Deng, Xiaoyun
- Cheng, Ran
- Ogasawara, Daisu ...
- Zhang, Genwei
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- Schafroth, Micha ...
- Dahl, Kenneth
- Fu, Hualong
- Hatori, Akiko
- Shao, Tuo
- Zhang, Yiding
- Yamasaki, Tomote ...
- Zhang, Xiaofei
- Rong, Jian
- Yu, Qngzhen
- Hu, Kuan
- Fujinaga, Masayu ...
- Xie, Lin
- Kumata, Katsushi
- Gou, Yuancheng
- Chen, Jingjin
- Gu, Shuyin
- Bao, Liang
- Wang, Lu
- Collier, Thomas ...
- Vasdev, Neil
- Shao, Yihan
- Ma, Jun-An
- Cravatt, Benjami ...
- Fowler, Christop ...
- Josephson, Lee
- Zhang, Ming-Rong
- Liang, Steven H.
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- MEDICAL AND HEALTH SCIENCES
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- Umeå University
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