{"created":"2023-05-15T14:37:30.884217+00:00","id":48389,"links":{},"metadata":{"_buckets":{"deposit":"8a6deac0-8b19-4c1d-b20b-1eaf7eb79fa3"},"_deposit":{"created_by":1,"id":"48389","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"48389"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00048389","sets":["1"]},"author_link":["486380","486391","486382","486374","486384","486368","486370","486385","486386","486369","486371","486377","486366","486383","486392","486389","486390","486367","486375","486388","486381","486376","486372","486365","486387","486373","486378","486379"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2017-06","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"56","bibliographicPageStart":"49","bibliographicVolumeNumber":"52","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Introduction: `The growth hormone secretagogue receptor 1a (GHS-R1a) is the orphan G-protein-coupled receptor,\nand its endogenous ligand is ghrelin. GHS-R1a contributes to regulation of glucose homeostasis,memory and learning,\nfood addiction, and neuroprotection. Several PET tracers for GHS-R1a have been developed, but none have been reported\nto be clinically applicable to GHS-R1a imaging. In this study, we developed three new PET tracers for GHSR1a:\n18F-labeled 6-(4-chlorophenyl)-3-((1-(2-fluoroethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-one\n(1), 11C-labeled 6-(4-chlorophenyl)-3-((1-(2-methoxyethyl)piperidin-3-yl)methyl)-2-(o-tolyl)quinazolin-4(3H)-\none (2), and 11C-labeled (S)-(4-(1H-indole-6-carbonyl)-3-methylpiperazin-1-yl)(4′-methoxy-[1,1′-biphenyl]-4-\nyl)methanone (3).\nMethods: [18F]1was synthesized by the 18F-fluoroethylation; [11C]2 or [11C]3 was synthesized by the 11C-methylation.\nBiodistribution studies and PET studies were conducted in mice.\nResults:Wesuccessfully radiosynthesized [18F]1, [11C]2, and[11C]3 with appropriate radioactivity for the animal study.\nIn the ex vivo biodistribution study, 60 min following injection, the radioactivity level of [18F]1 was relatively high in\nthe small intestine, that of [11C]2was high in the liver, and that of [11C]3was high in the pancreas. The radioactivity\nlevels of the three PET tracerswere relatively low in the brain. Under pretreatmentwith YIL781 (a selective and high\naffinity antagonist for GHS-R1a), the pancreas radioactivity level at 30min following [11C]3 injectionwas significantly\nreduced to 55% of control, but the radioactivity in the brain was not changed. In the PET study under control conditions,\nhigh radioactivity levels in the liver and pancreas were observed following [11C]3 injection. With YIL781 pretreatment,\nthe accumulated radioactivity in the pancreas 15–60 min after [11C]3 injection was significantly\ndecreased to 78% of control.\nConclusion: [11C]3 exhibited relatively high uptake and in vivo specific binding to GHS-R1a in the mouse pancreas.\n[11C]3 may be a useful PET tracers for in vivo imaging of GHS-R1a in the pancreas.","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.2017.06.002","subitem_relation_type_select":"DOI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0969-8051","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":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"486365","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"486366","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shimoda, Yoko"}],"nameIdentifiers":[{"nameIdentifier":"486367","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"486368","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"486369","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"486370","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"486371","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"486372","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"486373","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohkubo, Takayuki"}],"nameIdentifiers":[{"nameIdentifier":"486374","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurihara, Yusuke"}],"nameIdentifiers":[{"nameIdentifier":"486375","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"486376","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"486377","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"486378","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486379","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486380","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"下田 陽子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486381","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486382","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 一鼎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486383","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486384","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486385","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"脇坂 秀克","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486386","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486387","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"大久保 崇之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486388","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"栗原 雄祐","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486389","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"小川 政直","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486390","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486391","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"486392","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":"Developing new PET tracers to image the growth hormone secretagogue receptor 1a (GHS-R1a)","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Developing new PET tracers to image the growth hormone secretagogue receptor 1a (GHS-R1a)"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2017-11-30"},"publish_date":"2017-11-30","publish_status":"0","recid":"48389","relation_version_is_last":true,"title":["Developing new PET tracers to image the growth hormone secretagogue receptor 1a (GHS-R1a)"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:28:40.384056+00:00"}