{"created":"2023-05-15T14:53:55.409873+00:00","id":73424,"links":{},"metadata":{"_buckets":{"deposit":"aee0fcad-633a-4cd0-a214-2c37fabf87af"},"_deposit":{"created_by":1,"id":"73424","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"73424"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00073424","sets":["1"]},"author_link":["747428","747420","747419","747434","747436","747432","747418","747429","747435","747422","747430","747438","747426","747414","747427","747411","747417","747423","747421","747413","747431","747415","747412","747433","747416","747425","747437","747424"],"item_8_biblio_info_7":{"attribute_name":"書誌情報","attribute_value_mlt":[{"bibliographicIssueDates":{"bibliographicIssueDate":"2019-02","bibliographicIssueDateType":"Issued"},"bibliographicIssueNumber":"4","bibliographicVolumeNumber":"4","bibliographic_titles":[{"bibliographic_title":"EJNMMI Radiopharmacy and Chemistry"}]}]},"item_8_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Background: Neuropeptide Y (NPY) has been implicated in a wide variety of\nphysiological processes, including feeding, learning, memory, emotion, cardiovascular\nhomeostasis, hormone secretion, and circadian rhythms. NPY Yl receptor (NPY Y1-R) is\nthe most widely studied NPY receptor, and is involved in many of these processes.\nBMS-193885 (1) was previously developed as a potent and selective NPY Y1-R\nantagonist, which has good systemic bioavailability and brain penetration. To evaluate\nthe characteristics of 1 in vivo, we developed 11C-labeled BMS-193885 ([11C]1) and its\ndesmethyl analog ([11C]2) for potential use as two new positron emission tomography\n(PET) tracers.\nResults: [11C]1 was synthesized from [11C]methyl iodide using 2. [11C]2 was\nsynthesized from [11C]phosgene using its aniline and amine derivatives. The mean\n± S.D. decay-corrected radiochemical yields of [11C]1 and [11C]2 from 11CO2 at the\nend of radionuclide production were 23 ± 3.2% (n = 6) and 24 ± 1.5% (n = 4),\nrespectively. In biodistribution on mice, radioactivity levels for both tracers were\nrelatively high in the kidney, small intestine, and liver at 60 min post-injection. The\nradioactivity levels in the kidney, lung, and spleen of mice at 30 min post-injection\nwith [11C]1 were significantly reduced by pretreatment with 1 (10 mg/kg), and levels of\n[11C]1 in the brain of mice were significantly increased by pretreatment with the\nP-glycoprotein and breast cancer resistance protein inhibitor elacridar (10 mg/kg).\nIn metabolite analysis using mouse plasma, [11C]1 and [11C]2 were rapidly\nmetabolized within 30 min post-injection, and [11C]1 was mainly metabolized\ninto unlabeled 2 and radiolabeled components.\nConclusion: [11C]1 and [11C]2 were successfully synthesized with sufficient amount\nof radioactivity and high quality for use in vivo. Our study of [11C]1 and its desmethyl\nanalog [11C]2 was useful in that it helped to elucidate the in vivo characteristics of 1.\nKeywords: Carbon-11, Positron emission tomography, Neuropeptide Y1 receptor,\nBMS-193885","subitem_description_type":"Abstract"}]},"item_8_publisher_8":{"attribute_name":"出版者","attribute_value_mlt":[{"subitem_publisher":"Springer"}]},"item_8_relation_14":{"attribute_name":"DOI","attribute_value_mlt":[{"subitem_relation_type_id":{"subitem_relation_type_id_text":"10.1186/s41181-019-0056-5","subitem_relation_type_select":"DOI"}}]},"item_8_source_id_9":{"attribute_name":"ISSN","attribute_value_mlt":[{"subitem_source_identifier":"2365-421X","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":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"747411","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mori, Wakana"}],"nameIdentifiers":[{"nameIdentifier":"747412","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"747413","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"747414","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"747415","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"747416","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"747417","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"747418","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"747419","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohkubo, Takayuki"}],"nameIdentifiers":[{"nameIdentifier":"747420","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurihara, Yusuke"}],"nameIdentifiers":[{"nameIdentifier":"747421","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"747422","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"747423","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang"}],"nameIdentifiers":[{"nameIdentifier":"747424","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kawamura, Kazunori","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747425","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Mori, Wakana","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747426","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747427","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747428","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747429","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747430","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747431","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747432","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747433","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ohkubo, Takayuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747434","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kurihara, Yusuke","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747435","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747436","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747437","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ming-Rong, Zhang","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"747438","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":"Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":"Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors"}]},"item_type_id":"8","owner":"1","path":["1"],"pubdate":{"attribute_name":"公開日","attribute_value":"2019-02-20"},"publish_date":"2019-02-20","publish_status":"0","recid":"73424","relation_version_is_last":true,"title":["Radiosynthesis and in vivo evaluation of 11C-labeled BMS-193885 and its desmethyl analog as PET tracers for neuropeptide Y1 receptors"],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-16T01:12:19.507566+00:00"}