@article{oai:repo.qst.go.jp:00084582,
 author = {Rong, Jian and Wakana, Mori and Xia, Xiaotian and A. Schafroth, Michael and Zhao, Chunyu and S. Van, Richard and Tomoteru, Yamasaki and Chen, Jiahui and Xiao, Zhiwei and Haider, Ahmed and Ogasawara, Daisuke and Atsuto, Hiraishi and Shao, Tuo and Zhang, Yiding and Chen, Zhen and Pang, Fuwen and Kuan, Hu and Lin, Xie and Masayuki, Fujinaga and Katsushi, Kumata and Gou, Yuancheng and Fang, Yang and Gu, Shuyin and Wei, Huiyi and Bao, Liang and Xu, Hao and L. Collier, Thomas and Shao, Yihan and E. Carson, Richard and F. Cravatt, Benjamin and Lu, Wang and ming-rong, zhang and Liang, Huan and Wakana, Mori and Tomoteru, Yamasaki and Atsuto, Hiraishi and Zhang, Yiding and Kuan, Hu and Lin, Xie and Masayuki, Fujinaga and Katsushi, Kumata and Lu, Wang and Zhang, Ming-Rong and Liang, Huan},
 issue = {19},
 journal = {Journal of Medicinal Chemistry},
 month = {Oct},
 note = {Monoacylglycerol lipase (MAGL) is a 33 kDa serine protease primarily responsible for hydrolyzing 2-arachidonoylglycerol into the proinflammatory eicosanoid precursor arachidonic acid in the central nervous system. Inhibition of MAGL constitutes an attractive therapeutic concept for treating psychiatric disorders and neurodegenerative diseases. Herein, we present the design and synthesis of multiple reversible MAGL inhibitor candidates based on a piperazinyl azetidine scaffold. Compounds 10 and 15 were identified as the best-performing reversible MAGL inhibitors by pharmacological evaluations, thus channeling their radiolabeling with fluorine-18 in high radiochemical yields and favorable molar activity. Furthermore, evaluation of [18F]10 and [18F]15 ([18F]MAGL-2102) by autoradiography and positron emission tomography (PET) imaging in rodents and nonhuman primates demonstrated favorable brain uptakes, heterogeneous radioactivity distribution, good specific binding, and adequate brain kinetics, and [18F]15 demonstrated a better performance. In conclusion, [18F]15 was found to be a suitable PET radioligand for the visualization of MAGL, harboring potential for the successful translation into humans.},
 pages = {14283--14298},
 title = {Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold},
 volume = {64},
 year = {2021}
}