{"created":"2023-05-15T14:34:46.077292+00:00","id":44941,"links":{},"metadata":{"_buckets":{"deposit":"44a705cd-55f0-4467-90be-3d672d92d3c2"},"_deposit":{"created_by":1,"id":"44941","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"44941"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00044941","sets":["1"]},"author_link":["446302","446304","446303","446309","446305","446307","446308","446306"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2007-05","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"5","bibliographicPageEnd":"577","bibliographicPageStart":"571","bibliographicVolumeNumber":"34","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"The [18F]fluoromethyl analog of the sigma1 selective ligand 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503) ([18F]FM-SA4503) was prepared and its potential evaluated for the in vivo measurement of sigma1 receptors with positron emission tomography (PET). FM-SA4503 had selective affinity for the sigma1 receptor (Ki for sigma1 receptor, 6.4 nM; Ki for sigma2 receptor, 250 nM) that was compatible with the affinity of SA4503 (Ki for sigma1 receptor, 4.4 nM; Ki for sigma2 receptor, 242 nM). [18F]FM-SA4503 was synthesized by 18F-fluoromethylation of O-demethyl SA4503 in the radiochemical yield of 2.9-16.6% at the end of bombardment with a specific activity of 37.8-283 TBq/mmol at the end of synthesis. In mice, the uptake of [18F]FM-SA4503 in the brain was gradually increased for 30 min after injection, and then decreased. In the blocking study, brain uptake was significantly decreased by co-injection of haloperidol to 32% of control, and FM-SA4503 to 52% of control. In PET study of the monkey brain, high uptake was found in the cerebral cortex, thalamus and striatum. The radioactivity level of [18F]FM-SA4503 in the brain regions gradually increased over a period of 120 min after injection, followed by a stable plateau phase until 180 min after injection. In pretreatment with haloperidol measurement of the monkey brain, the radioactivity level was 22-32% and 11-25% of the baseline at 60 and 180 min, respectively, after injection, suggesting high receptor-specific binding. [18F]FM-SA4503 showed specific binding to sigma1 receptors in mice and monkeys; therefore, [18F]FM-SA4503 has the potential for mapping sigma1 receptors in the brain.","subitem_description_type":"Abstract"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1016/j.nucmedbio.2007.03.009","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":"446302","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tsukada, Hideo"}],"nameIdentifiers":[{"nameIdentifier":"446303","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shiba, Kazuhiro"}],"nameIdentifiers":[{"nameIdentifier":"446304","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kimura, Yuichi"}],"nameIdentifiers":[{"nameIdentifier":"446305","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ishiwata, Kiichi"}],"nameIdentifiers":[{"nameIdentifier":"446306","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"et.al"}],"nameIdentifiers":[{"nameIdentifier":"446307","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"木村 裕一","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"446308","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"石渡 喜一","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"446309","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 fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2007-08-15"},"publish_date":"2007-08-15","publish_status":"0","recid":"44941","relation_version_is_last":true,"title":["Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T00:09:32.386495+00:00"}