{"created":"2023-05-15T14:35:59.637901+00:00","id":46323,"links":{},"metadata":{"_buckets":{"deposit":"d3bfc5ef-3379-4283-8520-4135199f9052"},"_deposit":{"created_by":1,"id":"46323","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"46323"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00046323","sets":["1"]},"author_link":["461497","461505","461513","461489","461493","461490","461508","461510","461512","461488","461511","461503","461509","461498","461496","461495","461504","461492","461506","461494","461500","461502","461491","461507","461499","461501"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2012-02","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"5","bibliographicPageEnd":"2352","bibliographicPageStart":"2342","bibliographicVolumeNumber":"55","bibliographic_titles":[{"bibliographic_title":"Journal of Medicinal Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"We designed three novel positron emission tomography ligands, N-(4-(6-(isopropylamino)pyrimidin-4-yl)-1,3-\nthiazol-2-yl)-4-[11C]methoxy-N-methylbenzamide ([11C]6), 4-[18F]fluoroethoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-\nthiazol-2-yl]-N-methylbenzamide ([18F]7), and 4-[18F]fluoropropoxy-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-\nN-methylbenzamide ([18F]8), for imaging metabotropic glutamate receptor type 1 (mGluR1) in rodent brain. Unlabeled\ncompound 6 was synthesized by benzoylation of 4-pyrimidinyl-2-methylaminothiazole 10, followed by reaction with\nisopropylamine. Removal of the methyl group in 6 gave phenol precursor 12 for radiosynthesis. Two fluoroalkoxy analogues 7\nand 8 were prepared by reacting 12 with tosylates 13 and 14. Radioligands [11C]6, [18F]7, and [18F]8 were synthesized by\nO-[11C]methylation or [18F]fluoroalkylation of 12. Compound 6 showed high in vitro binding affinity for mGluR1, whereas 7 and 8\nhad weak affinity. Autoradiography using rat brain sections showed that [11C]6 binding is aligned with the reported distribution of\nmGluR1 with high specific binding in the cerebellum and thalamus. PET study with [11C]6 in rats showed high brain uptake and a\nsimilar distribution pattern to that in autoradiography, indicating the usefulness of [11C]6 for imaging brain mGluR1.","subitem_description_type":"Abstract"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1021/jm201590g","subitem_relation_type_select":"DOI"}}]},"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":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"461488","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"461489","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"461490","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"461491","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"461492","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"461493","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Asakawa, Chiharu"}],"nameIdentifiers":[{"nameIdentifier":"461494","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"461495","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yoshida, Yuichiro"}],"nameIdentifiers":[{"nameIdentifier":"461496","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"461497","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"461498","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fukumura, Toshimitsu"}],"nameIdentifiers":[{"nameIdentifier":"461499","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"461500","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461501","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461502","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461503","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461504","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461505","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461506","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"浅川 千春","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461507","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461508","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"吉田 勇一郎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461509","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"小川 政直","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461510","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461511","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"福村 利光","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461512","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"461513","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 Novel Radioligands for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rodent Brain","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Synthesis and Evaluation of Novel Radioligands for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rodent Brain"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2012-05-14"},"publish_date":"2012-05-14","publish_status":"0","recid":"46323","relation_version_is_last":true,"title":["Synthesis and Evaluation of Novel Radioligands for Positron Emission Tomography Imaging of Metabotropic Glutamate Receptor Subtype 1 (mGluR1) in Rodent Brain"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T23:53:13.268453+00:00"}