WEKO3
アイテム
{"_buckets": {"deposit": "2f336777-782c-4763-a62a-66e11ffb4b27"}, "_deposit": {"created_by": 1, "id": "47564", "owners": [1], "pid": {"revision_id": 0, "type": "depid", "value": "47564"}, "status": "published"}, "_oai": {"id": "oai:repo.qst.go.jp:00047564", "sets": ["1"]}, "author_link": ["476768", "476765", "476752", "476756", "476771", "476757", "476760", "476761", "476755", "476753", "476758", "476766", "476769", "476751", "476770", "476763", "476772", "476767", "476762", "476754", "476764", "476759"], "item_8_biblio_info_7": {"attribute_name": "書誌情報", "attribute_value_mlt": [{"bibliographicIssueDates": {"bibliographicIssueDate": "2016-10", "bibliographicIssueDateType": "Issued"}, "bibliographicIssueNumber": "11", "bibliographicPageEnd": "684", "bibliographicPageStart": "679", "bibliographicVolumeNumber": "43", "bibliographic_titles": [{"bibliographic_title": "Nuclear Medicine and Biology"}]}]}, "item_8_description_5": {"attribute_name": "抄録", "attribute_value_mlt": [{"subitem_description": "Introduction: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application.\nMethods: In manual synthesis, we optimized the reaction conditions of desmethyl precursor 2, which contains a 2-hydroxypyridine moiety, with [11C]MeI or [11C]MeOTf. After optimization, we performed automated synthesis and quality control of [11C]2.\nResults: Bubbling [11C]MeOTf into a heated mixture of precursor 1 and cesium carbonate in DMF at 100 °C for 90 sec produced [11C]2 with 7.9 ± 1.8 % (n = 78) of the radiochemical yields (decay-corrected, based on [11C]CO2). The specific activity of [11C]2 was 156 ± 52 GBq/mol (n = 78) at the end of synthesis. The total synthesis time was approximately 35 min from the end of bombardment. All the quality control results of [11C]2 were in compliance with our in-house quality control/assurance specifications. \nConclusion: We radiosynthesized [11C]TASP457 ([11C]2) with sufficient amounts of radioactivity and high quality for clinical usefulness. This radioligand is being used for PET assessment of H3 receptors in human brain in our facility.", "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.nucmedbio.2016.08.004", "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": "Hanyu, Masayuki"}], "nameIdentifiers": [{"nameIdentifier": "476751", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Kawamura, Kazunori"}], "nameIdentifiers": [{"nameIdentifier": "476752", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Takei, Makoto"}], "nameIdentifiers": [{"nameIdentifier": "476753", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Furutsuka, Kenji"}], "nameIdentifiers": [{"nameIdentifier": "476754", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Shiomi, Satoshi"}], "nameIdentifiers": [{"nameIdentifier": "476755", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fujishiro, Tomoya"}], "nameIdentifiers": [{"nameIdentifier": "476756", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Ogawa, Masanao"}], "nameIdentifiers": [{"nameIdentifier": "476757", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Nengaki, Nobuki"}], "nameIdentifiers": [{"nameIdentifier": "476758", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Hashimoto, Hiroki"}], "nameIdentifiers": [{"nameIdentifier": "476759", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Fukumura, Toshimitsu"}], "nameIdentifiers": [{"nameIdentifier": "476760", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "Zhang, Ming-Rong"}], "nameIdentifiers": [{"nameIdentifier": "476761", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "破入 正行", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476762", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "河村 和紀", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476763", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "武井 誠", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476764", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "古塚 賢士", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476765", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "潮見 聡", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476766", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "藤代 智也", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476767", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "小川 政直", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476768", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "念垣 信樹", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476769", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "橋本 裕輝", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476770", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "福村 利光", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476771", "nameIdentifierScheme": "WEKO"}]}, {"creatorNames": [{"creatorName": "張 明栄", "creatorNameLang": "en"}], "nameIdentifiers": [{"nameIdentifier": "476772", "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 quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain", "item_titles": {"attribute_name": "タイトル", "attribute_value_mlt": [{"subitem_title": "Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain"}]}, "item_type_id": "8", "owner": "1", "path": ["1"], "permalink_uri": "https://repo.qst.go.jp/records/47564", "pubdate": {"attribute_name": "公開日", "attribute_value": "2016-10-12"}, "publish_date": "2016-10-12", "publish_status": "0", "recid": "47564", "relation": {}, "relation_version_is_last": true, "title": ["Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain"], "weko_shared_id": -1}
Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain
https://repo.qst.go.jp/records/47564
https://repo.qst.go.jp/records/47564398627de-5e2f-4f2c-a836-235c8bfceff0
Item type | 学術雑誌論文 / Journal Article(1) | |||||
---|---|---|---|---|---|---|
公開日 | 2016-10-12 | |||||
タイトル | ||||||
タイトル | Radiosynthesis and quality control of [11C]TASP457 as a clinically useful PET ligand for imaging of histamine H3 receptors in human brain | |||||
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 |
Hanyu, Masayuki
× Hanyu, Masayuki× Kawamura, Kazunori× Takei, Makoto× Furutsuka, Kenji× Shiomi, Satoshi× Fujishiro, Tomoya× Ogawa, Masanao× Nengaki, Nobuki× Hashimoto, Hiroki× Fukumura, Toshimitsu× Zhang, Ming-Rong× 破入 正行× 河村 和紀× 武井 誠× 古塚 賢士× 潮見 聡× 藤代 智也× 小川 政直× 念垣 信樹× 橋本 裕輝× 福村 利光× 張 明栄 |
|||||
抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Introduction: Recently, 6-[(1-cyclobutylpiperidin-4-yl)oxy]- 1-(6-[11C]methoxypyridin-3-yl)-3,4-dihydroquinolin-2(1H)-one ([11C]TASP457, [11C]2) has been developed as a novel PET ligand for histamine H3 receptors in brain. [11C]2 is potentially suitable for imaging H3 receptors in rat and monkey brains, which has motivated us to perform first-in-human study of [11C]2 for qualifying H3 receptors in human brain. In this paper, we report efficient radiosynthesis of [11C]2 to obtain sufficient radioactivity and high quality for clinical application. Methods: In manual synthesis, we optimized the reaction conditions of desmethyl precursor 2, which contains a 2-hydroxypyridine moiety, with [11C]MeI or [11C]MeOTf. After optimization, we performed automated synthesis and quality control of [11C]2. Results: Bubbling [11C]MeOTf into a heated mixture of precursor 1 and cesium carbonate in DMF at 100 °C for 90 sec produced [11C]2 with 7.9 ± 1.8 % (n = 78) of the radiochemical yields (decay-corrected, based on [11C]CO2). The specific activity of [11C]2 was 156 ± 52 GBq/mol (n = 78) at the end of synthesis. The total synthesis time was approximately 35 min from the end of bombardment. All the quality control results of [11C]2 were in compliance with our in-house quality control/assurance specifications. Conclusion: We radiosynthesized [11C]TASP457 ([11C]2) with sufficient amounts of radioactivity and high quality for clinical usefulness. This radioligand is being used for PET assessment of H3 receptors in human brain in our facility. |
|||||
書誌情報 |
Nuclear Medicine and Biology 巻 43, 号 11, p. 679-684, 発行日 2016-10 |
|||||
出版者 | ||||||
出版者 | Elsevier | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1016/j.nucmedbio.2016.08.004 |