{"_buckets": {"deposit": "563fa7d4-bb6c-4b02-ba6a-20cd17d96c42"}, "_deposit": {"created_by": 1, "id": "75641", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "75641"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00075641", "sets": ["1"]}, "author_link": ["761490", "761510", "761485", "761491", "761505", "761479", "761494", "761519", "761499", "761488", "761512", "761493", "761495", "761492", "761487", "761503", "761513", "761515", "761496", "761483", "761518", "761521", "761507", "761480", "761517", "761478", "761504", "761481", "761497", "761482", "761477", "761516", "761514", "761498", "761520", "761501", "761508", "761511", "761506", "761486", "761509", "761500", "761502", "761489", "761484"], "item_8_biblio_info_7": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2019-03", "bibliographicIssueDateType": "Issued"}, "bibliographicIssueNumber": "7", "bibliographicPageEnd": "3353", "bibliographicPageStart": "3336", "bibliographicVolumeNumber": "62", "bibliographic_titles": [{"bibliographic_title": "Journal of Medicinal Chemistry"}]}]}, "item_8_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": " Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological conditions, including chronic pain, inflammation, cancer, and neurodegeneration. Herein, we disclose a novel array of reversible and irreversible MAGL inhibitors by means of “tail switching” on a piperazinyl azetidine scaffold. We developed a lead irreversible-binding MAGL inhibitor 8 and reversible-binding compounds 17 and 37, which are amenable for radiolabeling with 11C or18F. [11C]8 ([11C]MAGL-2-11) exhibited high brain uptake and excellent binding specificity in the brain toward MAGL. Reversible radioligands [11C]17 ([11C]PAD) and [18F]37 ([18F]MAGL-4-11) also demonstrated excellent in vivo binding specificity toward MAGL in peripheral organs. This work may pave the way for the development of MAGL-targeted positron emission tomography tracers with tunability in reversible and irreversible binding mechanisms. ", "subitem_description_type": "Abstract"}]}, "item_8_publisher_8": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "ACS Publications"}]}, "item_8_relation_14": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "10.1021/acs.jmedchem.8b01778", "subitem_relation_type_select": "DOI"}}]}, "item_8_relation_17": {"attribute_name": "関連サイト", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "https://pubs.acs.org/doi/10.1021/acs.jmedchem.8b01719", "subitem_relation_type_select": "URI"}}]}, "item_8_source_id_9": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "0022-2623", "subitem_source_identifier_type": "ISSN"}]}, "item_access_right": {"attribute_name": "アクセス権", "attribute_value_mlt": [{"subitem_access_right": "metadata only access", "subitem_access_right_uri": "http://purl.org/coar/access_right/c_14cb"}]}, "item_creator": {"attribute_name": "著者", "attribute_type": "creator", "attribute_value_mlt": [{"creatorNames": [{"creatorName": "Chen, Zhen"}], "nameIdentifiers": [{"nameIdentifier": "761477", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Mori, Wakana"}], "nameIdentifiers": [{"nameIdentifier": "761478", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Deng, Xiaoyun"}], "nameIdentifiers": [{"nameIdentifier": "761479", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Cheng, Ran"}], "nameIdentifiers": [{"nameIdentifier": "761480", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ogasawara, Daisuke"}], "nameIdentifiers": [{"nameIdentifier": "761481", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Genwei"}], "nameIdentifiers": [{"nameIdentifier": "761482", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "A. Schafroth, Michael"}], "nameIdentifiers": [{"nameIdentifier": "761483", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Dahl, Kenneth"}], "nameIdentifiers": [{"nameIdentifier": "761484", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fu, Hualong"}], "nameIdentifiers": [{"nameIdentifier": "761485", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hatori, Akiko"}], "nameIdentifiers": [{"nameIdentifier": "761486", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Shao, Tuo"}], "nameIdentifiers": [{"nameIdentifier": "761487", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding"}], "nameIdentifiers": [{"nameIdentifier": "761488", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yamasaki, Tomoteru"}], "nameIdentifiers": [{"nameIdentifier": "761489", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Xiaofei"}], "nameIdentifiers": [{"nameIdentifier": "761490", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Rong, Jian"}], "nameIdentifiers": [{"nameIdentifier": "761491", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yu, Qingzhen"}], "nameIdentifiers": [{"nameIdentifier": "761492", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kuan, Hu"}], "nameIdentifiers": [{"nameIdentifier": "761493", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujinaga, Masayuki"}], "nameIdentifiers": [{"nameIdentifier": "761494", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Xie, Lin"}], "nameIdentifiers": [{"nameIdentifier": "761495", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kumata, Katsushi"}], "nameIdentifiers": [{"nameIdentifier": "761496", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Gou, Yuancheng"}], "nameIdentifiers": [{"nameIdentifier": "761497", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Chen, Jingjin"}], "nameIdentifiers": [{"nameIdentifier": "761498", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Gu, Shuyin"}], "nameIdentifiers": [{"nameIdentifier": "761499", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Bao, Liang"}], "nameIdentifiers": [{"nameIdentifier": "761500", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Lu, Wang"}], "nameIdentifiers": [{"nameIdentifier": "761501", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Lee Collier, Thomas"}], "nameIdentifiers": [{"nameIdentifier": "761502", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Vasdev, Neil"}], "nameIdentifiers": [{"nameIdentifier": "761503", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Shao, Yihan"}], "nameIdentifiers": [{"nameIdentifier": "761504", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Jun-An, Ma"}], "nameIdentifiers": [{"nameIdentifier": "761505", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "F. Cravatt, Benjamin"}], "nameIdentifiers": [{"nameIdentifier": "761506", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fowler, Christopher"}], "nameIdentifiers": [{"nameIdentifier": "761507", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Josephson, Lee"}], "nameIdentifiers": [{"nameIdentifier": "761508", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ming-Rong, Zhang"}], "nameIdentifiers": [{"nameIdentifier": "761509", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Liang, Huan"}], "nameIdentifiers": [{"nameIdentifier": "761510", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Mori, Wakana", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761511", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hatori, Akiko", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761512", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761513", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yamasaki, Tomoteru", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761514", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kuan, Hu", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761515", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujinaga, Masayuki", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761516", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Xie, Lin", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761517", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kumata, Katsushi", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761518", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Lu, Wang", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761519", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ming-Rong, Zhang", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761520", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Liang, Huan", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "761521", "nameIdentifierScheme": "WEKO"}]}]}, "item_language": {"attribute_name": "言語", "attribute_value_mlt": [{"subitem_language": "eng"}]}, "item_resource_type": {"attribute_name": "資源タイプ", "attribute_value_mlt": [{"resourcetype": "journal article", "resourceuri": "http://purl.org/coar/resource_type/c_6501"}]}, "item_title": "Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton ", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton "}]}, "item_type_id": "8", "owner": "1", "path": ["1"], "permalink_uri": "https://repo.qst.go.jp/records/75641", "pubdate": {"attribute_name": "公開日", "attribute_value": "2019-04-18"}, "publish_date": "2019-04-18", "publish_status": "0", "recid": "75641", "relation": {}, "relation_version_is_last": true, "title": ["Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a “Tail Switching” Strategy on a Piperazinyl Azetidine Skeleton "], "weko_shared_id": -1}