{"_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"], "permalink_uri": "https://repo.qst.go.jp/records/73424", "pubdate": {"attribute_name": "公開日", "attribute_value": "2019-02-20"}, "publish_date": "2019-02-20", "publish_status": "0", "recid": "73424", "relation": {}, "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_shared_id": -1}