{"created":"2023-05-15T14:34:16.244241+00:00","id":44320,"links":{},"metadata":{"_buckets":{"deposit":"858880b8-79bd-4950-9522-6fb1ff47caa4"},"_deposit":{"created_by":1,"id":"44320","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"44320"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00044320","sets":["1"]},"author_link":["440227","440236","440230","440237","440240","440226","440241","440231","440234","440235","440239","440232","440238","440229","440228","440233"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2002","bibliographicIssueDateType":"Issued"},"bibliographicPageEnd":"476","bibliographicPageStart":"469","bibliographicVolumeNumber":"29","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"3-(4-Chlorobenzyl)-8-methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one (1), a putative dopamine D4 receptor antagonist (ki = 8.7 nM), was labeled by positron-emitter (11c) and its pharmacological evaluation was carried out with in vitro quantitative autoradiography and positron emission tomography (PET). 11C-Methylation of a corresponding desmethyl precursor (2) with [11C]CH3I gave [11C]1 with >98% of radiochemical purity after HPLC purification and 67_90 GBq/mumol of specific activity at the end of synthesis. The in vitro autoradiography using rat brain sections demonstrated that [11C]1 shows no specific binding to the D4 receptors, but a high specific binding to sigma1 receptors(IC50=105nM). In the PET study with monkey brain, [11C]1 was highly taken up by the brain and trapped in the brain for at least 90 min. The distribution pattern of radioactivity in the brain was striatum > thalamus > frontal cortex > cerebellum, which was same as the result of in vitro autoradiography. Pre-treatment with non-radioactive 1 (1 mg/kg) produced a significant reduction of radioactivity in all the regions including the cerebellum. Pre-treatment with (+)pentazocine  (1 mg/kg),a selective sigma1 receptor agonist, also reduced the radioactivity in the same regions to a similar extent. These results indicate that [11C]1 may have some specific binding to the sigma1 receptors, which is consistent with the result of in vitro autoradiography.","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":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"440226","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Haradahira, Terushi"}],"nameIdentifiers":[{"nameIdentifier":"440227","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Maeda, Jun"}],"nameIdentifiers":[{"nameIdentifier":"440228","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Okauchi, Takashi"}],"nameIdentifiers":[{"nameIdentifier":"440229","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawabe, Koichi"}],"nameIdentifiers":[{"nameIdentifier":"440230","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kida, Takayo"}],"nameIdentifiers":[{"nameIdentifier":"440231","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Obayashi, Shigeru"}],"nameIdentifiers":[{"nameIdentifier":"440232","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suzuki, Kazutoshi"}],"nameIdentifiers":[{"nameIdentifier":"440233","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Suhara, Tetsuya"}],"nameIdentifiers":[{"nameIdentifier":"440234","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440235","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"原田平 輝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440236","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"前田 純","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440237","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"岡内 隆","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440238","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"大林 茂","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440239","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"鈴木 和年","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440240","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"須原 哲也","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"440241","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 3-(4-chlorobenzyl)-8-[11C]methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one:a PET tracer for imaging sigma1 receptors","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and evaluation of 3-(4-chlorobenzyl)-8-[11C]methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one:a PET tracer for imaging sigma1 receptors"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2006-06-23"},"publish_date":"2006-06-23","publish_status":"0","recid":"44320","relation_version_is_last":true,"title":["Synthesis and evaluation of 3-(4-chlorobenzyl)-8-[11C]methoxy-1,2,3,4-tetrahydrochromeno[3,4-c]pyridin-5-one:a PET tracer for imaging sigma1 receptors"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T00:16:50.862135+00:00"}