{"created":"2023-05-15T14:37:44.101584+00:00","id":48680,"links":{},"metadata":{"_buckets":{"deposit":"f2ddef1d-de9f-4204-abbd-c1d566c9c04d"},"_deposit":{"created_by":1,"id":"48680","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"48680"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00048680","sets":["1"]},"author_link":["489768","489767","489772","489774","489773","489770","489771","489764","489769","489765","489766","489775","489776","489777"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2017-05","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"9","bibliographicPageEnd":"2565","bibliographicPageStart":"2558","bibliographicVolumeNumber":"106","bibliographic_titles":[{"bibliographic_title":"Journal of Pharmaceutical Sciences"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"We synthesized [11C]sulpiride as a positron emission tomography (PET) probe for investigating the drug distribution in the human body. [11C]Sulpiride was injected to healthy male subjects in either tracer dose of [11C]sulpiride (ca 222 MBq) or with therapeutic dose of sulpiride (500 mg, po) 3 hours prior to the injection in a crossover fashion. Whole body PET imaging demonstrated that [11C]sulpiride accumulated exceedingly in the bladder, followed by liver, gall bladder and kidney respectively; at 30 minutes after the injection, whereas scarcely in the brain. Oral dose of sulpiride decreased the hepatic accumulation of the radioactivity by 60%. From in vitro experiments, we found that sulpiride is a substrate of hOCT1 (Km 2.6μM), hOCT2 (Km 68μM), hMATE1 (Km 40μM) and hMATE2-K (Km 60μM). Moreover, the uptake of sulpiride by human hepatocytes was diminished by tetraethylammonium, and saturable with Km of 18 μM. Oct1/2 double knockout mice, and wild-type mice received Mate1 inhibitors (pyrimethamine/cimetidine) manifested reduced renal clearance of sulpiride, accompanied with its accumulation in the plasma. In conclusion, we found that sulpiride is a substrate of OCT1, OCT2, MATE1 and MATE2-K; and this suggests that [11C]sulpiride would be useful radiologand to investigate the organic cation transporters in humans.","subitem_description_type":"Abstract"}]},"item_8_relation_13":{"attribute_name":"PubMed番号","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"28499878","subitem_relation_type_select":"PMID"}}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1016/j.xphs.2017.05.006","subitem_relation_type_select":"DOI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0022-3549","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":"Takano, Harumasa"}],"nameIdentifiers":[{"nameIdentifier":"489764","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ito, Sumito"}],"nameIdentifiers":[{"nameIdentifier":"489765","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Xuan"}],"nameIdentifiers":[{"nameIdentifier":"489766","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ito, Hiroshi"}],"nameIdentifiers":[{"nameIdentifier":"489767","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"489768","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suzuki, Hiroshi"}],"nameIdentifiers":[{"nameIdentifier":"489769","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Kazuya"}],"nameIdentifiers":[{"nameIdentifier":"489770","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kusuhara, Hiroyuki"}],"nameIdentifiers":[{"nameIdentifier":"489771","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suhara, Tetsuya"}],"nameIdentifiers":[{"nameIdentifier":"489772","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sugiyama, Yuichi"}],"nameIdentifiers":[{"nameIdentifier":"489773","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"高野 晴成","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"489774","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"伊藤 浩","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"489775","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"489776","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"須原 哲也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"489777","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":"Possible role of organic cation transporters in the distribution of [11C]sulpiride, a dopamine D2 receptor antagonist","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Possible role of organic cation transporters in the distribution of [11C]sulpiride, a dopamine D2 receptor antagonist"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2018-04-08"},"publish_date":"2018-04-08","publish_status":"0","recid":"48680","relation_version_is_last":true,"title":["Possible role of organic cation transporters in the distribution of [11C]sulpiride, a dopamine D2 receptor antagonist"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:25:29.899477+00:00"}