{"created":"2023-05-15T14:36:08.659362+00:00","id":46526,"links":{},"metadata":{"_buckets":{"deposit":"f608b22a-817c-4582-b805-2cd06d1c287b"},"_deposit":{"created_by":1,"id":"46526","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"46526"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00046526","sets":["1"]},"author_link":["463662","463661","463660","463668","463666","463667","463663","463671","463670","463665","463669","463664"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2012-12","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"2","bibliographicPageEnd":"220","bibliographicPageStart":"214","bibliographicVolumeNumber":"40","bibliographic_titles":[{"bibliographic_title":"Nuclear Medicine and Biology"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Introduction\nPreclinical studies and first positron emission tomography (PET) imaging studies were performed using N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-4-[11C]methoxy-N-methylbenzamide ([11C]ITMM) to map metabotropic glutamate receptor type 1 (mGluR1) in the human brain.\nMethods\n[11C]ITMM was synthesized by O-methylation of the desmethyl precursor with [11C]methyl triflate in the presence of NaOH at room temperature. In vitro selectivity and brain distributions of [11C]ITMM in mice were characterized. Radiation absorbed-dose by [11C]ITMM in humans was calculated from mouse distribution data. Acute toxicity of ITMM at 4.72mg/kg body weight (>74,000-fold clinical equivalent dose of [11C]ITMM) was evaluated. Mutagenicity of ITMM was studied by the Ames test. Clinical PET imaging of mGluR1 with [11C] ITMM was performed in a healthy volunteer.\nResults\nITMM had low activity for a 28-standard receptor binding profile. Regional brain uptake of [11C]ITMM in mice was heterogeneous and consistent with known mGluR1 distributions. The radiation absorbed-dose by [11C]ITMM in humans was sufficiently low for clinical use, and no acute toxicity or mutagenicity of ITMM occurred. A 90-min dynamic PET scan with [11C]ITMM in a healthy volunteer showed a gradual increase of radioactivity in the cerebellum. Total distribution volume of [11C]ITMM was highest in the cerebellum, followed by thalamus, cerebral cortex, and striatum; regional differences in brain radioactivity corresponded to the mGluR1 distribution in the brain. Peripherally, [11C]ITMM was stable in humans: 60% of the plasma radioactivity remained in the unchanged form for 60min.\nConclusions\n[11C] ITMM is a suitable radioligand for imaging mGluR1 in the human brain providing acceptable dosimetry and pharmacological safety at the dose required for PET.","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.2012.11.008","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":"Toyohara, Jun"}],"nameIdentifiers":[{"nameIdentifier":"463660","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Sakata, Muneyuki"}],"nameIdentifiers":[{"nameIdentifier":"463661","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"463662","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"463663","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Oda, Keiichi"}],"nameIdentifiers":[{"nameIdentifier":"463664","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ishii, Kenji"}],"nameIdentifiers":[{"nameIdentifier":"463665","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"463666","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ishiwata, Kiichi"}],"nameIdentifiers":[{"nameIdentifier":"463667","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"豊原 潤","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"463668","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"463669","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"463670","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"463671","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":"Preclinical and the first clinical studies on [(11)C]ITMM for mapping metabotropic glutamate receptor subtype 1 by positron emission tomography.","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Preclinical and the first clinical studies on [(11)C]ITMM for mapping metabotropic glutamate receptor subtype 1 by positron emission tomography."}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2013-04-12"},"publish_date":"2013-04-12","publish_status":"0","recid":"46526","relation_version_is_last":true,"title":["Preclinical and the first clinical studies on [(11)C]ITMM for mapping metabotropic glutamate receptor subtype 1 by positron emission tomography."],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:50:43.140697+00:00"}