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PET imaging of fatty acid amide hydrolase in rat and monkey brains with 11C-MFTC
https://repo.qst.go.jp/records/71471
https://repo.qst.go.jp/records/71471b0e59789-1085-440f-b4f1-e0cc191f64dd
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2014-06-16 | |||||
| タイトル | ||||||
| タイトル | PET imaging of fatty acid amide hydrolase in rat and monkey brains with 11C-MFTC | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Kumata, Katsushi
× Kumata, Katsushi× Yui, Joji× Hatori, Akiko× Maeda, Jun× Ogawa, Masanao× Xie, Lin× Yamasaki, Tomoteru× Shimoda, Yoko× Fujinaga, Masayuki× Zhang, Ming-Rong× 熊田 勝志× 由井 譲二× 羽鳥 晶子× 前田 純× 小川 政直× 謝 琳× 山崎 友照× 下田 陽子× 藤永 雅之× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | 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. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | SNMMI 61th Annual Meeting | |||||
| 発表年月日 | ||||||
| 日付 | 2014-06-09 | |||||
| 日付タイプ | Issued | |||||
