量研学術機関リポジトリ「QST-Repository」は、国立研究開発法人 量子科学技術研究開発機構に所属する職員等が生み出した学術成果（学会誌発表論文、学会発表、研究開発報告書、特許等）を集積しインターネット上で広く公開するサービスです。 Welcome to QST-Repository where we accumulates and discloses the academic research results(Journal Publications, Conference presentation, Research and Development Report, Patent, etc.) of the members of National Institutes for Quantum and Radiological Science and Technology.
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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.
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
