{"created":"2023-05-15T15:01:01.106961+00:00","id":82773,"links":{},"metadata":{"_buckets":{"deposit":"900d2661-c44c-4297-a35d-735e17291323"},"_deposit":{"created_by":1,"id":"82773","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"82773"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00082773","sets":["1"]},"author_link":["1027067","1027061","1027060","1027056","1027055","1027054","1027065","1027068","1027064","1027066","1027057","1027063","1027058","1027062","1027059"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2021-03","bibliographicIssueDateType":"Issued"},"bibliographicPageStart":"153007","bibliographicVolumeNumber":"70","bibliographic_titles":[{"bibliographic_title":"Tetrahedron Letters"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Trace amine-associated receptor 1 (TAAR1) has been implicated in drug addiction, schizophrenia, depression and Parkinson’s disease (PD). To date, there are no reports on TAAR1-targeted probes for non-invasive quantification of receptor density in vivo. Herein, we report the synthesis of a 11C-labeled TAAR1 high-affinity antagonist N-(3-methoxyphenyl)-6-(pyrrolidin-1-yl)-5-(trifluoromethyl)nicotinamide [11C]4 (also named [11C]TAAR1-1911), as well as its physicochemical and preclinical evaluations for positron emission tomography (PET) imaging. This PET ligand was afforded using [11C]CH3I with the base NaOH in good radiochemical yield (non-decay corrected 14% relative to starting [11C]CO2), excellent radiochemical purities (> 99%) and high molar activities (> 37 GBq/µmol). Despite promising in vitro performance characteristics, [11C]4 did not exhibit in vivo specificity, potentially owing to fast metabolic degradation. Further studies are warranted to identify a suitable TAAR1 PET tracer, which would ultimately aid the development of TAAR1-directed therapeutic agents.","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":"10.1016/j.tetlet.2021.153007","subitem_relation_type_select":"DOI"}}]},"item_8_relation_17":{"attribute_name":"関連サイト","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"https://www.sciencedirect.com/science/article/abs/pii/S0040403921002033","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0040-4039","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":"Sun, Jiyun"}],"nameIdentifiers":[{"nameIdentifier":"1027054","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Chen, Jiahui"}],"nameIdentifiers":[{"nameIdentifier":"1027055","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsushi, Kumata"}],"nameIdentifiers":[{"nameIdentifier":"1027056","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xiao, Zhiwei"}],"nameIdentifiers":[{"nameIdentifier":"1027057","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Rong, Jiang"}],"nameIdentifiers":[{"nameIdentifier":"1027058","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Haider, Ahmed"}],"nameIdentifiers":[{"nameIdentifier":"1027059","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shao, Tuo"}],"nameIdentifiers":[{"nameIdentifier":"1027060","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lu, Wang"}],"nameIdentifiers":[{"nameIdentifier":"1027061","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xu, Hao"}],"nameIdentifiers":[{"nameIdentifier":"1027062","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"1027063","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Liang, Huan"}],"nameIdentifiers":[{"nameIdentifier":"1027064","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsushi, Kumata","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027065","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lu, Wang","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027066","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027067","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Liang, Huan","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027068","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":"Imaging the trace amine-associated receptor 1 by positron emission tomography","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Imaging the trace amine-associated receptor 1 by positron emission tomography"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2021-03-18"},"publish_date":"2021-03-18","publish_status":"0","recid":"82773","relation_version_is_last":true,"title":["Imaging the trace amine-associated receptor 1 by positron emission tomography"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T17:56:52.054248+00:00"}