{"created":"2023-05-15T14:35:37.155214+00:00","id":45806,"links":{},"metadata":{"_buckets":{"deposit":"be11e9cd-2565-47b9-81e6-78acf6c82351"},"_deposit":{"created_by":1,"id":"45806","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"45806"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00045806","sets":["1"]},"author_link":["455458","455472","455466","455457","455465","455470","455464","455467","455461","455469","455456","455473","455454","455460","455463","455455","455471","455462","455452","455468","455459","455453"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2010-06","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"5","bibliographicPageEnd":"412","bibliographicPageStart":"403","bibliographicVolumeNumber":"24","bibliographic_titles":[{"bibliographic_title":"Annals of Nuclear Medicine"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Objective  \nXR9576 (tariquidar) is an anthranilic acid derivative and potent P-glycoprotein (P-gp) inhibitor. XR9576 has undergone phase I and II studies as combined chemotherapy against cancer. XR9576 has been developed as a useful therapeutic agent but not as a PET probe. We therefore developed [11C]XR9576 as a PET probe and assessed whether PET studies using [11C]XR9576 are a promising approach to assess P-gp function primarily. \nMethods  \nWe synthesized [11C]XR9576 by methylation of 7-O-desmethyl XR9576 with [11C]methyl iodide. In in vivo tissue distribution, the effects of co-injection with XR9576 on the uptake of [11C]XR9576 in mice were investigated. PET studies using [11C]XR9576 were performed in P-gp and/or Bcrp knockout mice as well as in wild-type mice. Metabolites of [11C]XR9576 were measured in the brain and plasma of mice. \nResults  \n[11C]XR9576 was successfully synthesized with suitable radioactivity for injection as well as appropriate radiochemical purity and stability. In in vivo tissue distribution, the brain uptake of [11C]XR9576 significantly increased about tenfold of control on co-injection with >10 mg/kg of XR9576. In PET studies, the AUCbrain [0–60 min] in P-gp and P-gp/Bcrp knockout mice was 2- and 11-fold higher than that in wild-type mice. [11C]XR9576 showed a high metabolic stability (>90% unchanged form) in the brain and plasma of mice 30 min after injection. These results suggest that a tracer amount of [11C]XR9576 behave as the P-gp and Bcrp substrate, and the increased brain uptake or AUCbrain of [11C]XR9576 correlates with P-gp and Bcrp functions. \nConclusions  \nPET studies using [11C]XR9576 may be a promising approach for evaluating deficiency of the function of drug efflux transporters targeting intracranial diseases and tumors.","subitem_description_type":"Abstract"}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0914-7187","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":"455452","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Konno, Fujiko"}],"nameIdentifiers":[{"nameIdentifier":"455453","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"455454","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"455455","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"455456","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yanamoto, Kazuhiko"}],"nameIdentifiers":[{"nameIdentifier":"455457","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"455458","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Takei, Makoto"}],"nameIdentifiers":[{"nameIdentifier":"455459","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"455460","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fukumura, Toshimitsu"}],"nameIdentifiers":[{"nameIdentifier":"455461","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"455462","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455463","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"昆野 富士子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455464","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455465","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455466","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455467","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"柳本 和彦","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455468","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"脇坂 秀克","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455469","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"武井 誠","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455470","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455471","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"福村 利光","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455472","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"455473","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":"Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2010-06-16"},"publish_date":"2010-06-16","publish_status":"0","recid":"45806","relation_version_is_last":true,"title":["Synthesis and evaluation of [11C]XR9576 to assess the function of drug efflux transporters using PET"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:59:22.663506+00:00"}