{"created":"2023-05-15T14:37:17.048539+00:00","id":48072,"links":{},"metadata":{"_buckets":{"deposit":"4dcaffc3-073d-4634-beb7-13d081e12c96"},"_deposit":{"created_by":1,"id":"48072","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"48072"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00048072","sets":["1"]},"author_link":["733595","733599","733589","733587","733582","733584","733602","733586","733593","733598","733604","733600","733596","733583","733592","733597","733601","733585","733588","733603","733591","733605","733594","733590"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2017-04","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"9","bibliographicPageEnd":"4061","bibliographicPageStart":"4047","bibliographicVolumeNumber":"60","bibliographic_titles":[{"bibliographic_title":"Journal of Medicinal Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"We designed four novel acetamidobenzoxazolone compounds 7a–d as candidates of positron emission tomography (PET) radiotracers for imaging translocator protein (18 kDa, TSPO) in ischemic brain and glioma. Among these compounds, 2-(5-(6-fluoropyridin-3-yl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-methyl-N-phenylacetamide (7d) exhibited high binding affinity (Ki = 13.4 nM) with TSPO and moderate lipophilicity (cLogD: 1.92). [18F]7d was radiosynthesized by [18F]fluorination of the bromopyridine precursor 7h with [18F]F- at 9 ± 3% radiochemical yield (n = 15, decay-corrected). In vitro autoradiography and PET studies for ischemic rat brains showed significantly increased binding with TSPO on the ipsilateral side compared to the contralateral side. PET with [18F]7d showed improved brain kinetics than our radiotracers developed until now. Metabolite study of [18F]7d showed 93% of unchanged form in the ischemic brain at 30 min after radiotracer injection. Moreover, PET study with [18F]7d provided a clear tumor image in a glioma-bearing rat model. We demonstrated that [18F]7d is a useful PET radiotracer for visualization of not only neuroinflammation but also glioma and will translate this radiotracer to “first-in-human” study in our facility.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"ELSEVIER"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/acs.jmedchem.7b00374.","subitem_relation_type_select":"DOI"}}]},"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":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"733582","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Luo, Rui"}],"nameIdentifiers":[{"nameIdentifier":"733583","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"733584","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"733585","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"733586","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"733587","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"733588","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mori, Wakana"}],"nameIdentifiers":[{"nameIdentifier":"733589","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurihara, Yusuke"}],"nameIdentifiers":[{"nameIdentifier":"733590","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"733591","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"733592","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wang, Feng"}],"nameIdentifiers":[{"nameIdentifier":"733593","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang"}],"nameIdentifiers":[{"nameIdentifier":"733594","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733595","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733596","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733597","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733598","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733599","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733600","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mori, Wakana","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733601","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurihara, Yusuke","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733602","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733603","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733604","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"733605","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":"Development of a 18F-Labelled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Development of a 18F-Labelled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2017-06-21"},"publish_date":"2017-06-21","publish_status":"0","recid":"48072","relation_version_is_last":true,"title":["Development of a 18F-Labelled Radiotracer with Improved Brain Kinetics for Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain and Glioma"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T07:57:31.899955+00:00"}