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The aim of this study was to test the capability of [18F]T-401 for imaging MAGL in rat and monkey brains. \nMethods In vitro ARG was performed to evaluate [18F]T-401 binding to MAGL. [18F]T-401-PET imaging was conducted with and without pre-treatments with unlabeled T-401 and several doses of an MAGL inhibitor, JW642.\nResults ARG and PET demonstrated specific [18F]T-401 binding corresponding to MAGL distribution. [18F]T-401 kinetics was reversible and enabled estimation of total distribution volume (VT) in monkey brains. Pretreatment of monkeys with JW642 reduced VT values in a dose-dependent manner. 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新規モノアシルグリセロールリパーゼPETリガンド[18F]T-401の前臨床評価
https://repo.qst.go.jp/records/66981
https://repo.qst.go.jp/records/669819ac3a85c-2b6d-4daf-bea5-3b5b311644cd
Item type | 会議発表用資料 / Presentation(1) | |||||
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公開日 | 2018-11-19 | |||||
タイトル | ||||||
タイトル | 新規モノアシルグリセロールリパーゼPETリガンド[18F]T-401の前臨床評価 | |||||
言語 | ||||||
言語 | jpn | |||||
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 |
関, 千江
× 関, 千江× 服部, 靖志× 前田, 純× 永井, 裕司× 内田, 翔子× 徳永, 正希× 張, 明栄× 小池竜樹× 樋口, 真人× 関 千江× 服部 靖志× 前田 純× 永井 裕司× 内田 翔子× 徳永 正希× 張 明栄× 樋口 真人 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Introduction Monoacylglycerol lipase (MAGL) is considered as a novel therapeutic target of CNS disorders. [18F]T-401 has been developed as a reversible and selective PET imaging agent. The aim of this study was to test the capability of [18F]T-401 for imaging MAGL in rat and monkey brains. Methods In vitro ARG was performed to evaluate [18F]T-401 binding to MAGL. [18F]T-401-PET imaging was conducted with and without pre-treatments with unlabeled T-401 and several doses of an MAGL inhibitor, JW642. Results ARG and PET demonstrated specific [18F]T-401 binding corresponding to MAGL distribution. [18F]T-401 kinetics was reversible and enabled estimation of total distribution volume (VT) in monkey brains. Pretreatment of monkeys with JW642 reduced VT values in a dose-dependent manner. Conclusion The current observations support the utility of [18F]T-401 for quantitative PET evaluation of MAGL. |
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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 | 第58回日本核医学会学術総会に参加し武田薬品との共同研究成果を発表 | |||||
発表年月日 | ||||||
日付 | 2018-11-15 | |||||
日付タイプ | Issued |