{"_buckets": {"deposit": "6b554f4f-a451-4232-9f37-b8fe4ef5aa0a"}, "_deposit": {"created_by": 1, "id": "48777", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "48777"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00048777", "sets": ["1"]}, "author_link": ["491110", "491115", "491114", "491107", "491113", "491101", "491094", "491088", "491089", "491106", "491116", "491112", "491098", "491090", "491102", "491109", "491104", "491105", "491092", "491118", "491111", "491121", "491108", "491120", "491086", "491084", "491097", "491096", "491093", "491100", "491095", "491099", "491117", "491103", "491087", "491119", "491091", "491085"], "item_8_biblio_info_7": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2017-08", "bibliographicIssueDateType": "Issued"}, "bibliographicIssueNumber": "63", "bibliographicVolumeNumber": "7", "bibliographic_titles": [{"bibliographic_title": "EJNMMI Research"}]}]}, "item_8_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Background: α-Amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor is a primary mediator of fast\nglutamatergic excitatory signaling in the brain and has been implicated in diverse neuropsychiatric diseases. We\nrecently developed a novel positron emission tomography (PET) ligand, 2-(1-(3-([11C]methylamino)phenyl)-2-oxo-5-\n(pyrimidin-2-yl)-1,2-dihydropyridin-3-yl) benzonitrile ([11C]HMS011). This compound is a radiolabelled derivative of\nperampanel, an antiepileptic drug acting on AMPA receptors, and was demonstrated to have promising in vivo\nproperties in the rat and monkey brains. In the current study, we performed a human PET study using [11C]HMS011\nto evaluate its safety and kinetics.\nFour healthy male subjects underwent a 120-min PET scan after injection of [11C]HMS011. Arterial blood sampling\nand metabolite analysis were performed to obtain parent input functions for three of the subjects using highperformance\nliquid chromatography. Regional distribution volumes (VTs) were calculated based on kinetic models\nwith and without considering radiometabolite in the brain. The binding was also quantified using a reference tissue\nmodel with white matter as reference.\nResults: Brain uptake of [11C]HMS011 was observed quickly after the injection, followed by a rapid clearance. Three\nhydrophilic and one lipophilic radiometabolites appeared in the plasma, with notable individual variability. The kinetics\nin the brain with apparent radioactivity retention suggested that the lipophilic radiometabolite could enter the brain. A\ndual-input graphical model, an analytical model designed in consideration of a radiometabolite entering the brain, well\ndescribed the kinetics of [11C]HMS011. A reference tissue model showed small radioligand binding potential (BP*ND)\nvalues in the cortical regions (BP*ND = 0–0.15). These data suggested specific binding component of [11C]HMS011 in\nthe brain.\nConclusions: Kinetic analyses support some specific binding of [11C]HMS011 in the human cortex. However, this ligand\nmay not be suitable for practical AMPA receptor PET imaging due to the small dynamic range and metabolite in the brain.\nKeywords: PET, Perampanel, AMPA, [11C]HMS011, Interspecies differences", "subitem_description_type": "Abstract"}]}, "item_8_publisher_8": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "Springer Berlin"}]}, "item_8_relation_13": {"attribute_name": "PubMed番号", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "28815446", "subitem_relation_type_select": "PMID"}}]}, "item_8_relation_14": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "10.1186/s13550-017-0313-0", "subitem_relation_type_select": "DOI"}}]}, "item_8_source_id_9": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "2191-219X", "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": "Takahata, Keisuke"}], "nameIdentifiers": [{"nameIdentifier": "491084", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kimura, Yasuyuki"}], "nameIdentifiers": [{"nameIdentifier": "491085", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Seki, Chie"}], "nameIdentifiers": [{"nameIdentifier": "491086", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Tokunaga, Masaki"}], "nameIdentifiers": [{"nameIdentifier": "491087", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ichise, Masanori"}], "nameIdentifiers": [{"nameIdentifier": "491088", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kawamura, Kazunori"}], "nameIdentifiers": [{"nameIdentifier": "491089", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ono, Maiko"}], "nameIdentifiers": [{"nameIdentifier": "491090", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kitamura, Soichiro"}], "nameIdentifiers": [{"nameIdentifier": "491091", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kubota, Manabu"}], "nameIdentifiers": [{"nameIdentifier": "491092", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Moriguchi, Sho"}], "nameIdentifiers": [{"nameIdentifier": "491093", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ishii, Tatsuya"}], "nameIdentifiers": [{"nameIdentifier": "491094", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Takado, Yuhei"}], "nameIdentifiers": [{"nameIdentifier": "491095", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Niwa, Fumitoshi"}], "nameIdentifiers": [{"nameIdentifier": "491096", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Endo, Hironobu"}], "nameIdentifiers": [{"nameIdentifier": "491097", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nagashima, Tomohisa"}], "nameIdentifiers": [{"nameIdentifier": "491098", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ikoma, Yoko"}], "nameIdentifiers": [{"nameIdentifier": "491099", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Ming-Rong"}], "nameIdentifiers": [{"nameIdentifier": "491100", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Suhara, Tetsuya"}], "nameIdentifiers": [{"nameIdentifier": "491101", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Higuchi, Makoto"}], "nameIdentifiers": [{"nameIdentifier": "491102", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "高畑 圭輔", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491103", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "木村 泰之", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491104", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "関 千江", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491105", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "徳永 正希", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491106", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "市瀬 正則", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491107", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "河村 和紀", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491108", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "小野 麻衣子", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491109", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "北村 聡一郎", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491110", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "久保田 学", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491111", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "森口 翔", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491112", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "石井 辰弥", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491113", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "高堂 裕平", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491114", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "丹羽 文俊", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491115", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "遠藤 浩信", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491116", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "永嶌 朋久", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491117", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "生駒 洋子", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491118", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 明栄", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491119", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "須原 哲也", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491120", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "樋口 真人", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "491121", "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": "A human PET study of [¹¹C]HMS011, a potential radioligand for AMPA receptors", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "A human PET study of [¹¹C]HMS011, a potential radioligand for AMPA receptors"}]}, "item_type_id": "8", "owner": "1", "path": ["1"], "permalink_uri": "https://repo.qst.go.jp/records/48777", "pubdate": {"attribute_name": "公開日", "attribute_value": "2018-04-23"}, "publish_date": "2018-04-23", "publish_status": "0", "recid": "48777", "relation": {}, "relation_version_is_last": true, "title": ["A human PET study of [¹¹C]HMS011, a potential radioligand for AMPA receptors"], "weko_shared_id": -1}