WEKO3
アイテム
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Compound 1 showed a high binding affinity for FAAH\n(IC50: 3.3 nM). [11C]1 was synthesized by reaction of 5-amino-3,4-dimethylisoxazole (2) with [11C]\nphosgene ([11C]COCl2), followed by reaction with 4-(4-fluorophenyl)-2-(piperazin-1-yl)thiazole (3), with\na 9 4% radiochemical yield (decay-corrected, n ¼ 9) based on [11C]CO2. A biodistribution study in\nmice showed a high uptake of radioactivity in FAAH-rich organs, including the lung, liver, and kidney.\nPET summation images of rat brains showed high radioactivity (\u003e2 SUV) in the cerebellar nuclei and\nfrontal cortex. This pattern was consistent with the known regional distribution pattern of FAAH in the\nrodent brain. Pretreatment with the FAAH-selective inhibitor URB597 significantly reduced the whole\nbrain uptake of [11C]1. At 30 min after the radiotracer injection, more than 95% of the total radioactivity\nwas found to be irreversible in the brain homogenate of rats. 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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
https://repo.qst.go.jp/records/47381
https://repo.qst.go.jp/records/4738166b4d238-ccf8-4cb7-9d1c-ff4a7e563cbb
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2016-01-18 | |||||
タイトル | ||||||
タイトル | 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 | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Shimoda, Yoko
× Shimoda, Yoko× Yui, Joji× Zhang, Yiding× Hatori, Akiko× Ogawa, Masanao× Fujinaga, Masayuki× Yamasaki, Tomoteru× Xie, Lin× Kumata, Katsushi× Zhang, Ming-Rong× 下田 陽子× 由井 譲二× 張 一鼎× 羽鳥 晶子× 小川 政直× 藤永 雅之× 山崎 友照× 謝 琳× 熊田 勝志× 張 明栄 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 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. |
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書誌情報 |
RSC Advances 巻 5, p. 106122-106127, 発行日 2015-12 |