{"created":"2023-05-15T14:47:55.404731+00:00","id":65682,"links":{},"metadata":{"_buckets":{"deposit":"56aca15e-9414-46c8-adfe-01d0aa4b53ba"},"_deposit":{"created_by":1,"id":"65682","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"65682"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00065682","sets":["10:29"]},"author_link":["647024","647025","647020","647023","647021","647026","647027","647008","647015","647009","647017","647014","647029","647028","647019","647016","647018","647010","647013","647012","647011","647022"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2015-06-10","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Objectives: Overexpression of metabotropic glutamate1 receptor (mGlu1) is found in brain and various cancers (1). Recently, we constructed the first mGlu1 oncoprotein-based PET platform with mGlu1-specific radioprobe 18F-FITM (2). However, 18F-FITM displayed high uptake of radioactivity both in brain and melanoma, which increased the risk of radiation-induced brain injury, then hampered its clinical application. In this study, using FITM as a lead compound, we developed a novel PET probe 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-11C-methyl- benzamide (11C-IITM) and explored its potential for melanoma imaging.\nMethods: 11C-IITM was synthesized by N-11C-methylation of the desmethyl precursor with 11C-CH3OTf. In vitro binding affinity for mGlu1 was assayed. PET imaging and biodistribution were performed in the mice bearing B16F10 melanoma with rich mGlu1 expression.\nResults: 11C-IITM was obtained with radiochemical yields of 20  5% (n > 10 based on 11C-CO2, EOS), radiochemical purity of >97%, and specific activity of 65–160 GBq/mol. PET showed high accumulation of radioactivity in target tumor (4.0 % ID/g) and very low uptake in non-target brain (0.9 % ID/g) in B16F10-bearing mice at 75 min after 11C-IITM injection. Ex vivo biodistribution confirmed the PET images and indicated better uptake ratio of tumor to brain in 11C-IITM (8.03 ± 0.46), compared with 18F-FITM (0.58 ± 0.05) at 90 min. In addition, the ratios of radioactivity for 11C-IITM in the tumor compared to blood, skin, and muscle at 90 min were 5-10. Treatment with  an mGlu1 selective ligand significantly reduced radioactive uptake in the tumor. \nConclusions: 11C-IITM is a useful PET tracer for mGlu1 imaging in melanoma. This radioprobe can be further developed by 124I and 131I labeling for long-duration PET scan and radiotherapeutic usage.","subitem_description_type":"Abstract"}]},"item_10005_description_6":{"attribute_name":"会議概要（会議名, 開催地, 会期, 主催者等）","attribute_value_mlt":[{"subitem_description":"SNMMI 2015 Annual Meeting ","subitem_description_type":"Other"}]},"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":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"647008","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"647009","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"647010","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"647011","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shimoda, Yoko"}],"nameIdentifiers":[{"nameIdentifier":"647012","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"647013","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"647014","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"647015","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"647016","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"647017","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"647018","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647019","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647020","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647021","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647022","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"下田 陽子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647023","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647024","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647025","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 一鼎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647026","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647027","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647028","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"647029","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":"conference object","resourceuri":"http://purl.org/coar/resource_type/c_c94f"}]},"item_title":"Developing 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N- 11C-methylbenzamide for imaging of metabotropic glutamate 1 receptor in melanoma ","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Developing 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N- 11C-methylbenzamide for imaging of metabotropic glutamate 1 receptor in melanoma "}]},"item_type_id":"10005","owner":"1","path":["29"],"pubdate":{"attribute_name":"公開日","attribute_value":"2015-06-17"},"publish_date":"2015-06-17","publish_status":"0","recid":"65682","relation_version_is_last":true,"title":["Developing 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N- 11C-methylbenzamide for imaging of metabotropic glutamate 1 receptor in melanoma "],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T20:57:25.456425+00:00"}