{"created":"2023-05-15T14:59:32.672199+00:00","id":80793,"links":{},"metadata":{"_buckets":{"deposit":"1dfc1b28-9bf6-4d09-bf54-a3fa0514fed4"},"_deposit":{"created_by":1,"id":"80793","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"80793"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00080793","sets":["1"]},"author_link":["1027186","1027192","1027206","1027184","1027199","1027188","1027197","1027200","1027205","1027189","1027182","1027179","1027204","1027209","1027183","1027201","1027210","1027202","1027191","1027208","1027198","1027203","1027180","1027193","1027187","1027195","1027196","1027207","1027190","1027185","1027178","1027194","1027181"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2020-09","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"63","bibliographicPageEnd":"11483","bibliographicPageStart":"11469","bibliographicVolumeNumber":"2020","bibliographic_titles":[{"bibliographic_title":"Journal of Medicinal Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Metabotropic glutamate receptor 2 (mGlu2) is a known target for treating several central nervous system (CNS) disorders. To develop a viable positron emission tomography (PET) ligand for mGlu2, we identified new candidates 5a–i that are potent negative allosteric modulators (NAMs) of mGlu2. Among these candidates, 4-(2-fluoro-4-methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide (5i, also named as [11C]MG2-1812) exhibited high potency, high subtype selectivity, and favorable lipophilicity. Compound 5i was labeled with positron-emitting carbon-11 (11C) to obtain [11C]5i in high radiochemical yield and high molar activity by O-[11C]methylation of the phenol precursor 12 with [11C]CH3I. In vitro autoradiography with [11C]5i showed heterogeneous radioactive accumulation in the brain tissue sections, ranked in the order: cortex > striatum > hippocampus > cerebellum ≫ thalamus > pons. PET study of [11C]5i indicated in vivo specific binding of mGlu2 in the rat brain. Based on the [11C]5i scaffold, further optimization for new candidates is underway to identify a more suitable ligand for imaging mGlu2.","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"ACS Publications"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/acs.jmedchem.9b01991","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://pubs.acs.org/doi/10.1021/acs.jmedchem.9b01991","subitem_relation_type_select":"URI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"0022-2623","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":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"1027178","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Xiaofei"}],"nameIdentifiers":[{"nameIdentifier":"1027179","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"1027180","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"1027181","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Deng, Xiaoyun"}],"nameIdentifiers":[{"nameIdentifier":"1027182","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"1027183","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Chen, Zhen"}],"nameIdentifiers":[{"nameIdentifier":"1027184","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mori, Wakana"}],"nameIdentifiers":[{"nameIdentifier":"1027185","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu"}],"nameIdentifiers":[{"nameIdentifier":"1027186","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"1027187","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"1027188","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"1027189","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"1027190","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"1027191","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Van, Richard"}],"nameIdentifiers":[{"nameIdentifier":"1027192","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shao, Yihan"}],"nameIdentifiers":[{"nameIdentifier":"1027193","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"J. Sheffler, Douglas"}],"nameIdentifiers":[{"nameIdentifier":"1027194","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"D. P. Cosford, Nicholas"}],"nameIdentifiers":[{"nameIdentifier":"1027195","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Liang, Huan"}],"nameIdentifiers":[{"nameIdentifier":"1027196","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang"}],"nameIdentifiers":[{"nameIdentifier":"1027197","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Tomoteru, Yamasaki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027198","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Katsushi, Kumata","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027199","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027200","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masayuki, Fujinaga","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027201","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakana, Mori","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027202","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kuan, Hu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027203","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hidekatsu, Wakizaka","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027204","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Akiko, Hatori","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027205","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Lin, Xie","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027206","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Masanao, Ogawa","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027207","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nobuki, Nengaki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027208","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Liang, Huan","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027209","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"1027210","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":"Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2)","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2)"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2020-10-09"},"publish_date":"2020-10-09","publish_status":"0","recid":"80793","relation_version_is_last":true,"title":["Identification and Development of a New Positron Emission Tomography Ligand 4-(2-Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for Imaging Metabotropic Glutamate Receptor Subtype 2 (mGlu2)"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T17:56:32.908121+00:00"}