WEKO3
アイテム
{"_buckets": {"deposit": "97762870-65e2-46d4-84bb-babfa2066090"}, "_deposit": {"created_by": 1, "id": "49007", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "49007"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00049007", "sets": ["1"]}, "author_link": ["494216", "494219", "494217", "494221", "494211", "494212", "494218", "494220", "494202", "494215", "494208", "494203", "494204", "494207", "494210", "494205", "494209", "494213", "494206", "494214"], "item_8_biblio_info_7": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2018-02", "bibliographicIssueDateType": "Issued"}, "bibliographicPageEnd": "8", "bibliographicPageStart": "1", "bibliographicVolumeNumber": "150", "bibliographic_titles": [{"bibliographic_title": "European Journal of Medicinal Chemistry"}]}]}, "item_8_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Translocator Protein (18 kDa, TSPO) is regarded as a useful biomarker for neuroinflammation imaging. TSPO PET imaging could be used to understand the role of neuroinflammation in brain diseases and as a tool for evaluating novel therapeutic effects. As a promising TSPO probe, [18F]DPA-714 is highly specific and offers reliable quantification of TSPO in vivo. In this study, we further radiosynthesized and evaluated another novel TSPO probe, 2-(7-butyl-2-(4-(2-[18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide ([18F]VUIIS1018A), which features a 700-fold higher binding affinity for TSPO than that of [18F]DPA-714. We evaluated the performance of [18F]VUIIS1018A using dynamic in vivo PET imaging, radiometabolite analysis, in vitro autoradiography assays, biodistribution analysis, and blocking assays. In vivo study using this probe demonstrated high signal-to-noise ratio, binding potential (BPND), and binding specificity in preclinical neuroinflammation studies. Taken together, these findings indicate that [18F]VUIIS1018A may serve as a novel TSPO PET probe for neuroinflammation imaging.", "subitem_description_type": "Abstract"}]}, "item_8_publisher_8": {"attribute_name": "出版者", "attribute_value_mlt": [{"subitem_publisher": "Elsevier"}]}, "item_8_relation_14": {"attribute_name": "DOI", "attribute_value_mlt": [{"subitem_relation_type_id": {"subitem_relation_type_id_text": "10.1016/j.ejmech.2018.02.076", "subitem_relation_type_select": "DOI"}}]}, "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": "Tang, Dewei"}], "nameIdentifiers": [{"nameIdentifier": "494202", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujinaga, Masayuki"}], "nameIdentifiers": [{"nameIdentifier": "494203", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hatori, Akiko"}], "nameIdentifiers": [{"nameIdentifier": "494204", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Yiding"}], "nameIdentifiers": [{"nameIdentifier": "494205", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Yamasaki, Tomoteru"}], "nameIdentifiers": [{"nameIdentifier": "494206", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Xie, Lin"}], "nameIdentifiers": [{"nameIdentifier": "494207", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Mori, Wakana"}], "nameIdentifiers": [{"nameIdentifier": "494208", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kumata, Katsushi"}], "nameIdentifiers": [{"nameIdentifier": "494209", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Liu, Jianjun"}], "nameIdentifiers": [{"nameIdentifier": "494210", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Charles, Manning H."}], "nameIdentifiers": [{"nameIdentifier": "494211", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Huang, Gang"}], "nameIdentifiers": [{"nameIdentifier": "494212", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Ming-Rong"}], "nameIdentifiers": [{"nameIdentifier": "494213", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "藤永 雅之", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494214", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "羽鳥 晶子", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494215", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 一鼎", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494216", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "山崎 友照", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494217", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "謝 琳", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494218", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "森 若菜", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494219", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "熊田 勝志", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494220", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 明栄", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "494221", "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": "Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation"}]}, "item_type_id": "8", "owner": "1", "path": ["1"], "permalink_uri": "https://repo.qst.go.jp/records/49007", "pubdate": {"attribute_name": "公開日", "attribute_value": "2018-05-15"}, "publish_date": "2018-05-15", "publish_status": "0", "recid": "49007", "relation": {}, "relation_version_is_last": true, "title": ["Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation"], "weko_shared_id": -1}
Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation
https://repo.qst.go.jp/records/49007
https://repo.qst.go.jp/records/49007cf2e57ec-9bce-418b-af45-69960ac6b647
Item type | 学術雑誌論文 / Journal Article(1) | |||||
---|---|---|---|---|---|---|
公開日 | 2018-05-15 | |||||
タイトル | ||||||
タイトル | Evaluation of the novel TSPO radiotracer 2-(7-butyl-2-(4-(2-([18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide in a preclinical model of neuroinflammation | |||||
言語 | ||||||
言語 | eng | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
アクセス権 | ||||||
アクセス権 | metadata only access | |||||
アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
著者 |
Tang, Dewei
× Tang, Dewei× Fujinaga, Masayuki× Hatori, Akiko× Zhang, Yiding× Yamasaki, Tomoteru× Xie, Lin× Mori, Wakana× Kumata, Katsushi× Liu, Jianjun× Charles, Manning H.× Huang, Gang× Zhang, Ming-Rong× 藤永 雅之× 羽鳥 晶子× 張 一鼎× 山崎 友照× 謝 琳× 森 若菜× 熊田 勝志× 張 明栄 |
|||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Translocator Protein (18 kDa, TSPO) is regarded as a useful biomarker for neuroinflammation imaging. TSPO PET imaging could be used to understand the role of neuroinflammation in brain diseases and as a tool for evaluating novel therapeutic effects. As a promising TSPO probe, [18F]DPA-714 is highly specific and offers reliable quantification of TSPO in vivo. In this study, we further radiosynthesized and evaluated another novel TSPO probe, 2-(7-butyl-2-(4-(2-[18F]fluoroethoxy)phenyl)-5-methylpyrazolo[1,5-a]pyrimidin-3-yl)-N,N-diethylacetamide ([18F]VUIIS1018A), which features a 700-fold higher binding affinity for TSPO than that of [18F]DPA-714. We evaluated the performance of [18F]VUIIS1018A using dynamic in vivo PET imaging, radiometabolite analysis, in vitro autoradiography assays, biodistribution analysis, and blocking assays. In vivo study using this probe demonstrated high signal-to-noise ratio, binding potential (BPND), and binding specificity in preclinical neuroinflammation studies. Taken together, these findings indicate that [18F]VUIIS1018A may serve as a novel TSPO PET probe for neuroinflammation imaging. | |||||
書誌情報 |
European Journal of Medicinal Chemistry 巻 150, p. 1-8, 発行日 2018-02 |
|||||
出版者 | ||||||
出版者 | Elsevier | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.ejmech.2018.02.076 |