@misc{oai:repo.qst.go.jp:00071471,
 author = {Kumata, Katsushi and Yui, Joji and Hatori, Akiko and Maeda, Jun and Ogawa, Masanao and Xie, Lin and Yamasaki, Tomoteru and Shimoda, Yoko and Fujinaga, Masayuki and Zhang, Ming-Rong and 熊田 勝志 and 由井 譲二 and 羽鳥 晶子 and 前田 純 and 小川 政直 and 謝 琳 and 山崎 友照 and 下田 陽子 and 藤永 雅之 and 張 明栄},
 month = {Jun},
 note = {Fatty acid amide hydrolase (FAAH) is a hydrolyzing enzyme which converts anandamide to arachidonic acid and ethanolamine. It has been reported that the selective inhibitors of FAAH show evident pharmacological effects on pain, anxiety, addiction, and psychiatric disorders. There are two PET radiotracers for FAAH which have been used in human brain. The first clinically-used PET tracer for FAAH is 11C-CURB (Fig. 1), an irreversible inhibitor for FAAH. This radiotracer is  an analog of the FAAH-selective inhibitor URB597 (Fig. 1) and contains a carbamate moiety necessary for expressing FAAH activity, in which the carbonyl group was labeled with 11C, has been used to measure FAAH activity in human brains.
The objective of this study is to develop a novel radiotracer containing an 11C-carbonyl-carbamate moiety for PET imaging of FAAH in rat and monkey brains, with expectation that this tracer can be used to visualize FAAH in human brain. Our present targeted compound is 2-methylpyridin-3-yl-4-(5-(2-fluorophenyl)-4H-1,2,4-triazol-3-yl)piperidine-1-carboxylate (MFTC, Fig. 2) which was reported to show high binding affinity for FAAH in a preliminary in vitro binding assay. Because of the arylcarbamate structure, this compound could be assumed as an irreversible inhibitor for FAAH, like CURB and URB597.
In this study, we synthesized the novel radiotracer 11C-MFTC using 11C-phosgene (11C-COCl2) as a labeling agent and 11C-carbonate as an intermediate (Fig. 2). We evaluated the potentials of 11C-MFTC as a PET imaging agent for FAAH in rat and monkey brains by determining in vitro binding affinity and biodistribution, and performing PET scans., SNMMI 61th Annual Meeting},
 title = {PET imaging of fatty acid amide hydrolase in rat and monkey brains with 11C-MFTC},
 year = {2014}
}