@article{oai:repo.qst.go.jp:00075641,
 author = {Chen, Zhen and Mori, Wakana and Deng, Xiaoyun and Cheng, Ran and Ogasawara, Daisuke and Zhang, Genwei and A. Schafroth, Michael and Dahl, Kenneth and Fu, Hualong and Hatori, Akiko and Shao, Tuo and Zhang, Yiding and Yamasaki, Tomoteru and Zhang, Xiaofei and Rong, Jian and Yu, Qingzhen and Kuan, Hu and Fujinaga, Masayuki and Xie, Lin and Kumata, Katsushi and Gou, Yuancheng and Chen, Jingjin and Gu, Shuyin and Bao, Liang and Lu, Wang and Lee Collier, Thomas and Vasdev, Neil and Shao, Yihan and Jun-An, Ma and F. Cravatt, Benjamin and Fowler, Christopher and Josephson, Lee and Ming-Rong, Zhang and Liang, Huan and Mori, Wakana and Hatori, Akiko and Zhang, Yiding and Yamasaki, Tomoteru and Kuan, Hu and Fujinaga, Masayuki and Xie, Lin and Kumata, Katsushi and Lu, Wang and Ming-Rong, Zhang and Liang, Huan},
 issue = {7},
 journal = {Journal of Medicinal Chemistry},
 month = {Mar},
 note = {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.},
 pages = {3336--3353},
 title = {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},
 volume = {62},
 year = {2019}
}