{"created":"2023-05-15T14:52:32.067992+00:00","id":71725,"links":{},"metadata":{"_buckets":{"deposit":"ee905f41-ec7a-4890-90f6-6a3f80a1275d"},"_deposit":{"created_by":1,"id":"71725","owners":[1],"pid":{"revision_id":0,"type":"depid","value":"71725"},"status":"published"},"_oai":{"id":"oai:repo.qst.go.jp:00071725","sets":["10:28"]},"author_link":["705838","705856","705850","705841","705863","705840","705861","705860","705849","705847","705845","705844","705852","705854","705858","705843","705864","705842","705851","705859","705848","705846","705839","705865","705857","705853","705862","705855"],"item_10005_date_7":{"attribute_name":"発表年月日","attribute_value_mlt":[{"subitem_date_issued_datetime":"2015-05-27","subitem_date_issued_type":"Issued"}]},"item_10005_description_5":{"attribute_name":"抄録","attribute_value_mlt":[{"subitem_description":"Objectives: The I2-imidazoline receptor (I2R) is involved in various neuropsychiatric disorders, but the these function\nare unknown. In addition, selective I2R ligands promote food intake and may therefore alter eating behavior. The\ncarrier dose of PET ligand may modify both binding and pharmacokinetics in small animal imaging studies. Ultra-high\nspecific activity (SA) is a useful tool to investigate a receptor with low density and small region in the brain [1]. We\nrecently reported that [11C]FTIMD with ultra-high SA (mean 4470 GBq/μmol) for imaging of I2Rs showed higher\nspecific-binding than [11C]FTIMD with conventional SA (about 100 GBq/μmol) in the hypothalamus, which is highly\nexpressed I2Rs [2]. More recently, Kealey et al. developed [11C]BU99008 as a more potent PET ligand for I2R\nimaging [3]. [11C]BU99008 displayed a relatively high brain penetration and specific binding in the porcine and rhesus\nbrain [3,4]. In this study, to image I2Rs in extremely small region such as hypothalamus, we synthesized and\nevaluated [11C]BU99008 with ultra-high SA as a PET ligand.\nMethods: [11C]BU99008 was prepared by methylation of the BU-precursor and [11C]methyl iodide. In case of ultrahigh\nSA, [11C]methyl iodide was produced by iodination of [11C]methane using the single-pass method [1,2].\nBiodistribution and brain PET studies were conducted in rats.\nResults: [11C]BU99008 with conventional and ultra-high SA were successfully synthesized in the range of SA at\n55∼220 [n = 8] and 5400∼16600 [n = 7] GBq/μmol at the end of synthesis, respectivery, yielding a radioactivity\nsuitable for injection. In PET studies, the radioactivity after injection of [11C]BU99008 with conventional or ultra-high\nSA was highly accumulated in the hypothalamus. Pretreatment with BU224 (an high affinity I2R ligand; 1 mg/kg)\nsignificantly decreased the radioactivity (AUC30-60 min) of conventional or ultra-high SA in the hypothalamus to 76%\nor 86% of the correspoding control radioactivity (AUC30-60 min), respectively.\nConclusions: [11C]BU99008 with ultra-high SA showed high specific binding in rat brain. PET study using [11\nC]BU99008 with ultra-high SA would contribute to the detection of I2Rs expression in small regions or with small\nchange.\nReferences: [1] Noguchi J, et al (2003), Nucl Med Biol, 30, 335-43. [2] Kawamura K, et al (2012), Nucl Med Biol, 39,\n199-206. [3] Kealey S, et al (2013), J Nucl Med, 54, 139-44. [4] Parker CA, et al (2014), J Nucl Med, 55, 838-44.\n(No Image Selected)","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":"21st International Symposium on Radiopharmaceutical Sciences","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":"Kawamura, Kazunori"}],"nameIdentifiers":[{"nameIdentifier":"705838","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Shimoda, Yoko"}],"nameIdentifiers":[{"nameIdentifier":"705839","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yui, Joji"}],"nameIdentifiers":[{"nameIdentifier":"705840","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Fujinaga, Masayuki"}],"nameIdentifiers":[{"nameIdentifier":"705841","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yamasaki, Tomoteru"}],"nameIdentifiers":[{"nameIdentifier":"705842","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Hatori, Akiko"}],"nameIdentifiers":[{"nameIdentifier":"705843","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Xie, Lin"}],"nameIdentifiers":[{"nameIdentifier":"705844","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Yiding"}],"nameIdentifiers":[{"nameIdentifier":"705845","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Kumata, Katsushi"}],"nameIdentifiers":[{"nameIdentifier":"705846","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Ogawa, Masanao"}],"nameIdentifiers":[{"nameIdentifier":"705847","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Yusuke, Kurihara"}],"nameIdentifiers":[{"nameIdentifier":"705848","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Nengaki, Nobuki"}],"nameIdentifiers":[{"nameIdentifier":"705849","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Wakizaka, Hidekatsu"}],"nameIdentifiers":[{"nameIdentifier":"705850","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"Zhang, Ming-Rong"}],"nameIdentifiers":[{"nameIdentifier":"705851","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"河村 和紀","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705852","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"下田 陽子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705853","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"由井 譲二","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705854","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"藤永 雅之","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705855","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"山崎 友照","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705856","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"羽鳥 晶子","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705857","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"謝 琳","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705858","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 一鼎","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705859","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"熊田 勝志","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705860","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"小川 政直","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705861","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"栗原 雄祐","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705862","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"念垣 信樹","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705863","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"脇坂 秀克","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705864","nameIdentifierScheme":"WEKO"}]},{"creatorNames":[{"creatorName":"張 明栄","creatorNameLang":"en"}],"nameIdentifiers":[{"nameIdentifier":"705865","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":" Radiosynthesis and evaluation of [11C]BU99008 with ultra-high specific activity as a PET ligand for imaging I2-imidazoline receptors.","item_titles":{"attribute_name":"タイトル","attribute_value_mlt":[{"subitem_title":" Radiosynthesis and evaluation of [11C]BU99008 with ultra-high specific activity as a PET ligand for imaging I2-imidazoline receptors."}]},"item_type_id":"10005","owner":"1","path":["28"],"pubdate":{"attribute_name":"公開日","attribute_value":"2015-06-15"},"publish_date":"2015-06-15","publish_status":"0","recid":"71725","relation_version_is_last":true,"title":[" Radiosynthesis and evaluation of [11C]BU99008 with ultra-high specific activity as a PET ligand for imaging I2-imidazoline receptors."],"weko_creator_id":"1","weko_shared_id":-1},"updated":"2023-05-15T19:48:04.743474+00:00"}