{"created":"2023-05-15T14:36:58.681737+00:00","id":47652,"links":{},"metadata":{"_buckets":{"deposit":"bc374010-f001-431e-bd29-0d9a22b3e8cd"},"_deposit":{"created_by":1,"id":"47652","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"47652"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00047652","sets":["1"]},"author_link":["477963","477961","477973","477960","477954","477957","477953","477974","477956","477967","477950","477947","477969","477958","477949","477965","477962","477959","477952","477968","477951","477955","477964","477972","477948","477971","477970","477966"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2016-02","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"1","bibliographicPageStart":"11","bibliographicVolumeNumber":"6","bibliographic_titles":[{"bibliographic_title":"EJNMMI Research"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Background: Histamine H3 receptor (H3R) is a potential therapeutic target of sleep- and cognition-related disorders. The purpose of the present study is to develop a novel positron emission tomography (PET) ligand for H3Rs from dihydroquinolinone derivatives, which we previously found to have high affinity with these receptors.\nMethods: Six compounds were selected from a dihydroquinolinone compound library based on structural capability for 11C labeling and binding affinity for H3Rs. Their in-vivo kinetics in the rat brain were examined in a comparative manner by liquid chromatography and tandem mass spectrometry (LC-MS/MS). Chemicals with appropriate kinetic properties were then labeled with 11C and evaluated in rats and monkeys using PET. \nResults: Of the six compounds, TASP0410457 (also diminutively called TASP457) and TASP0434988 exhibited fast kinetics and relatively high brain uptakes in ex vivo LC-MS/MS, and were selected as candidate PET imaging agents. PET data in rat brains were mostly consistent with LC-MS/MS findings, and rat and monkey PET scans demonstrated that [11C]TASP0410457 was superior to [11C]TASP0434988 for high-contrast H3R PET imaging. In the monkey brain PET, distribution volume for [11C]TASP0410457 could be quantified, and receptor occupancy by nonradioactive compounds was measurable using this radioligand. The specific binding of [11C]TASP0410457 to H3Rs was confirmed by autoradiography using rat and monkey brain sections.\nConclusions: We developed [11C]TASP0410457 as a radioligand enabling a robust quantification of H3Rs in all brain regions, and demonstrated the utility of ex vivo LC-MS/MS and in vivo PET assays for selecting appropriate imaging tracers. [11C]TASP0410457 will help to examine the implication of H3Rs in neuropsychiatric disorders and to characterize emerging therapeutic agents targeting H3Rs.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Springer"}]},"item_8_relation_13":{"attribute_name":"PubMed番号","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"26860293","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/s13550-016-0170-2","subitem_relation_type_select":"DOI"}}]},"item_8_relation_17":{"attribute_name":"関連サイト","attribute_value_mlt":[{"subitem_relation_name":[{"subitem_relation_name_text":"http://www.ejnmmires.com/content/6/1/11"}],"subitem_relation_type_id":{"subitem_relation_type_id_text":"http://www.ejnmmires.com/content/6/1/11","subitem_relation_type_select":"URI"}}]},"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 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Toshio"}],"nameIdentifiers":[{"nameIdentifier":"477953","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nagai, Yuji"}],"nameIdentifiers":[{"nameIdentifier":"477954","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Seki, Chie"}],"nameIdentifiers":[{"nameIdentifier":"477955","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kimura, Yasuyuki"}],"nameIdentifiers":[{"nameIdentifier":"477956","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Minamimoto, Takafumi"}],"nameIdentifiers":[{"nameIdentifier":"477957","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"477958","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fukumura, Toshimitsu"}],"nameIdentifiers":[{"nameIdentifier":"477959","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suhara, Tetsuya"}],"nameIdentifiers":[{"nameIdentifier":"477960","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Higuchi, Makoto"}],"nameIdentifiers":[{"nameIdentifier":"477961","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"古閑 一実","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477962","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 純","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477963","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"徳永 正希","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477964","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"破入 正行","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477965","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477966","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"永井 裕司","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477967","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"関 千江","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477968","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"木村 泰之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477969","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"南本 敬史","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477970","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477971","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"福村 利光","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477972","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"須原 哲也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477973","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"樋口 真人","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"477974","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":"Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2017-03-08"},"publish_date":"2017-03-08","publish_status":"0","recid":"47652","relation_version_is_last":true,"title":["Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:37:08.038489+00:00"}