@article{oai:repo.qst.go.jp:00047381,
 author = {Shimoda, Yoko and Yui, Joji and Zhang, Yiding and Hatori, Akiko and Ogawa, Masanao and Fujinaga, Masayuki and Yamasaki, Tomoteru and Xie, Lin and Kumata, Katsushi and Zhang, Ming-Rong and 下田 陽子 and 由井 譲二 and 張 一鼎 and 羽鳥 晶子 and 小川 政直 and 藤永 雅之 and 山崎 友照 and 謝 琳 and 熊田 勝志 and 張 明栄},
 journal = {RSC Advances},
 month = {Dec},
 note = {We developed a novel positron emission tomography (PET) radiotracer N-(3,4-dimethylisoxazol-5-yl)
piperazine-4-[4-(4-fluorophenyl)thiazol-2-yl]-1-[11C]carboxamide ([11C]DPFC, [11C]1) for in vivo imaging
of fatty acid amide hydrolase (FAAH) in rat brain. Compound 1 showed a high binding affinity for FAAH
(IC50: 3.3 nM). [11C]1 was synthesized by reaction of 5-amino-3,4-dimethylisoxazole (2) with [11C]
phosgene ([11C]COCl2), followed by reaction with 4-(4-fluorophenyl)-2-(piperazin-1-yl)thiazole (3), with
a 9   4% radiochemical yield (decay-corrected, n ¼ 9) based on [11C]CO2. A biodistribution study in
mice showed a high uptake of radioactivity in FAAH-rich organs, including the lung, liver, and kidney.
PET summation images of rat brains showed high radioactivity (>2 SUV) in the cerebellar nuclei and
frontal cortex. This pattern was consistent with the known regional distribution pattern of FAAH in the
rodent brain. Pretreatment with the FAAH-selective inhibitor URB597 significantly reduced the whole
brain uptake of [11C]1. At 30 min after the radiotracer injection, more than 95% of the total radioactivity
was found to be irreversible in the brain homogenate of rats. Our results indicate that [11C]1 is
a promising PET tracer for in vivo visualization of FAAH in living brains.},
 pages = {106122--106127},
 title = {Radiosynthesis and evaluation of N-(3,4-dimethylisoxazol-5-yl)piperazine-4-[4-(4- fluorophenyl)thiazol-2-yl]-1-[11C]carboxamide for in vivo positron emission tomography imaging of fatty acid amide hydrolase in brain},
 volume = {5},
 year = {2015}
}