{"created":"2023-05-15T14:36:54.801150+00:00","id":47564,"links":{},"metadata":{"_buckets":{"deposit":"2f336777-782c-4763-a62a-66e11ffb4b27"},"_deposit":{"created_by":1,"id":"47564","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"47564"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00047564","sets":["1"]},"author_link":["476768","476765","476752","476756","476771","476757","476760","476761","476755","476753","476758","476766","476769","476751","476770","476763","476772","476767","476762","476754","476764","476759"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2016-10","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"11","bibliographicPageEnd":"684","bibliographicPageStart":"679","bibliographicVolumeNumber":"43","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Introduction: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application.\nMethods: In manual synthesis, we optimized the reaction conditions of desmethyl precursor 2, which contains a 2-hydroxypyridine moiety, with [11C]MeI or [11C]MeOTf. After optimization, we performed automated synthesis and quality control of [11C]2.\nResults: Bubbling [11C]MeOTf into a heated mixture of precursor 1 and cesium carbonate in DMF at 100 °C for 90 sec produced [11C]2 with 7.9 ± 1.8 % (n = 78) of the radiochemical yields (decay-corrected, based on [11C]CO2). The specific activity of [11C]2 was 156 ± 52 GBq/mol (n = 78) at the end of synthesis. The total synthesis time was approximately 35 min from the end of bombardment. All the quality control results of [11C]2 were in compliance with our in-house quality control/assurance specifications. \nConclusion: We radiosynthesized [11C]TASP457 ([11C]2) with sufficient amounts of radioactivity and high quality for clinical usefulness. This radioligand is being used for PET assessment of H3 receptors in human brain in our facility.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Elsevier"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1016/j.nucmedbio.2016.08.004","subitem_relation_type_select":"DOI"}}]},"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":"Hanyu, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"476751","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"476752","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takei, Makoto"}],"nameIdentifiers":[{"nameIdentifier":"476753","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Furutsuka, Kenji"}],"nameIdentifiers":[{"nameIdentifier":"476754","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shiomi, Satoshi"}],"nameIdentifiers":[{"nameIdentifier":"476755","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujishiro, Tomoya"}],"nameIdentifiers":[{"nameIdentifier":"476756","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"476757","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"476758","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hashimoto, Hiroki"}],"nameIdentifiers":[{"nameIdentifier":"476759","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fukumura, Toshimitsu"}],"nameIdentifiers":[{"nameIdentifier":"476760","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"476761","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"破入 正行","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476762","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476763","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"武井 誠","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476764","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"古塚 賢士","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476765","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"潮見 聡","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476766","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤代 智也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476767","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"小川 政直","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476768","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476769","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"橋本 裕輝","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476770","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"福村 利光","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476771","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"476772","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":"Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2016-10-12"},"publish_date":"2016-10-12","publish_status":"0","recid":"47564","relation_version_is_last":true,"title":["Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:38:17.504996+00:00"}