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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) | |||||
|---|---|---|---|---|---|---|
| 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 |
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