{"created":"2023-05-15T14:34:59.413582+00:00","id":45201,"links":{},"metadata":{"_buckets":{"deposit":"7905d8cd-eca4-4071-b680-aa27ea9c1b1c"},"_deposit":{"created_by":1,"id":"45201","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"45201"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00045201","sets":["1"]},"author_link":["448976","448987","448978","448983","448989","448984","448991","448981","448982","448988","448986","448990","448992","448985","448977","448980","448994","448979","448993"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2008-02","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"2","bibliographicPageEnd":"212","bibliographicPageStart":"203","bibliographicVolumeNumber":"35","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"High-affinity iodine- and ethyl-C-5 substituted analogs of 4-hydroxy-3-(3-[11C]methoxyphenyl)-2(1H)-quinolone ([11C]4HQ) were synthesized as new positron emission tomography radioligands for the glycine-binding sites of the N-methyl-d-aspartate (NMDA) ion channel. Although both radioligands showed high in vitro specific binding to rat brain slices, their binding characteristics were quite different from each other. 5-Ethyl-[11C]4HQ (5Et-[11C]4HQ) showed higher in vitro binding in the forebrain regions than in the cerebellum, bindings that were strongly inhibited by both glycine-site agonists and antagonists. In contrast, 5-iodo-[11C]4HQ (5I-[11C]4HQ) showed a homogeneous in vitro binding throughout the brain, which was inhibited by antagonists but not by agonists. This difference in in vitro binding between 5Et-[11C]4HQ and 5I-[11C]4HQ was quite similar to that previously observed between [11C]L-703,717 and [11C]4HQ, both glycine-site antagonists. In vivo brain uptakes of these 11C-labeled 4-hydroxyquinolones were examined in mice. Initial brain uptakes of 5Et- and 5I-[11C]4HQ at 1 min after intravenous injections were comparable to that of [11C]4HQ, but they were 1.3-2.1 times higher than that of [11C]L-703,717. The treatment with an anticoagulant, warfarin, only slightly increased the initial uptakes of [11C]4HQ and 5Et-[11C]4HQ in contrast to [11C]L-703,717. The in vivo regional brain distributions were slightly different between the two radioligands. Pretreatment with nonradioactive ligand (2 mg/kg) slightly inhibited the binding of 5Et-[11C]4HQ (16-36% inhibition) but not that of 5I-[11C]4HQ. In this study, it was found that a small structural change in [11C]4HQ resulted in a major change in binding characteristics and distributions, suggesting the existence of two binding sites for [11C]4-hydroxyquinolones on the NMDA ion channel - agonist-sensitive and agonist-insensitive (or antagonist-preferring) sites.","subitem_description_type":"Abstract"}]},"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":"Fuchigami, Takeshi"}],"nameIdentifiers":[{"nameIdentifier":"448976","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Haradahira, Terushi"}],"nameIdentifiers":[{"nameIdentifier":"448977","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujimoto, Noriko"}],"nameIdentifiers":[{"nameIdentifier":"448978","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Okauchi, Takashi"}],"nameIdentifiers":[{"nameIdentifier":"448979","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Jun"}],"nameIdentifiers":[{"nameIdentifier":"448980","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suzuki, Kazutoshi"}],"nameIdentifiers":[{"nameIdentifier":"448981","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suhara, Tetsuya"}],"nameIdentifiers":[{"nameIdentifier":"448982","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamamoto, Fumihiko"}],"nameIdentifiers":[{"nameIdentifier":"448983","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mukai, Takahiro"}],"nameIdentifiers":[{"nameIdentifier":"448984","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Magata, Yasuhiro"}],"nameIdentifiers":[{"nameIdentifier":"448985","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Minoru"}],"nameIdentifiers":[{"nameIdentifier":"448986","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"et.al"}],"nameIdentifiers":[{"nameIdentifier":"448987","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"淵上 剛志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448988","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"原田平 輝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448989","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"岡内 隆","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448990","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 純","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448991","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"鈴木 和年","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448992","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"須原 哲也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448993","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 稔","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"448994","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":"Difference in brain distribustions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Difference in brain distribustions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2008-06-17"},"publish_date":"2008-06-17","publish_status":"0","recid":"45201","relation_version_is_last":true,"title":["Difference in brain distribustions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T00:06:28.865996+00:00"}