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Of the two geometric isomers of ABP688, (E)-\nABP688 has a greater affinity towards mGlu5 receptors than (Z)-ABP688. Therefore, a high ratio of E-isomer is\nrequired when using [11C]ABP688 as a PET probe for imaging and quantification of mGlu5 receptors. The aim\nof this study was to evaluate the effect (Z)-[11C]ABP688 on the synthesis of [11C]ABP688 to be used for binding\n(E)-[11C]ABP688 in the brain.\nMethods: We synthesized and separated (E)- and (Z)-[11C]ABP688 by purification using an improved\npreparative high-performance liquid chromatography (HPLC) method equipped with a COSMOSIL Cholester\ncolumn. We performed an in vitro binding assay in rat brain homogenates and PET studies of the rat brains\nusing (E)- and (Z)-[11C]ABP688.\nResults: (E)- and (Z)-[11C]ABP688 were successfully obtained with suitable radioactivity for application. In the\nin vitro assay, the Kd value of (E)-[11C]ABP688 (5.7 nmol/L) was higher than that of (Z)-[11C]ABP688 (140\nnmol/L). In the PET study of the rat brain, high radioactivity after injection of (E)-[11C]ABP688 was observed in\nregions rich in mGlu5 receptors such as the striatum and hippocampus. In contrast, after injection of (Z)-[11C]\nABP688, radioactivity did not accumulate in the brain. Furthermore, BPND in the striatum and hippocampus\nwas highly correlated (R2=0.99) with the percentage of (E)-[11C]ABP688 of the total radioactivity of (E)- and\n(Z)-[11C]ABP688 in the injection.\nConclusion: We demonstrated that including (Z)-[11C]ABP688 in the [11C]ABP688 injection can decrease BPND\nin regions rich in mGlu5 receptors. Routine production of (E)-[11C]ABP688 will be helpful for imaging and\nquantification of mGlu5 receptors in clinical studies.", "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": "doi.org/10.1016/j.nucmedbio.2013.09.008", "subitem_relation_type_select": "DOI"}}]}, "item_8_source_id_9": {"attribute_name": "ISSN", "attribute_value_mlt": [{"subitem_source_identifier": "0969-8051", "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, 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Binding potential of (E)-[11C]ABP688 to metabotropic glutamate receptor subtype 5 is decreased by the inclusion of its 11C-labelled Z-isomer
https://repo.qst.go.jp/records/46746
https://repo.qst.go.jp/records/467466ff8d9d2-417d-49bb-81d7-f814723deecd
Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2014-03-18 | |||||
タイトル | ||||||
タイトル | Binding potential of (E)-[11C]ABP688 to metabotropic glutamate receptor subtype 5 is decreased by the inclusion of its 11C-labelled Z-isomer | |||||
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 |
Kawamura, Kazunori
× Kawamura, Kazunori× Yamasaki, Tomoteru× Kumata, Katsushi× Furutsuka, Kenji× Takei, Makoto× Wakizaka, Hidekatsu× Fujinaga, Masayuki× Kaori, Kariya× Yui, Joji× Hatori, Akiko× Xie, Lin× Shimoda, Yoko× Hashimoto, Hiroki× Hayashi, Kazutaka× Zhang, Ming-Rong× 河村 和紀× 山崎 友照× 熊田 勝志× 古塚 賢士× 武井 誠× 脇坂 秀克× 藤永 雅之× 由井 譲二× 羽鳥 晶子× 謝 琳× 下田 陽子× 橋本 裕輝× 林 和孝× 張 明栄 |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | Introduction: [11C]ABP688 is a promising positron emission tomography (PET) ligand for imaging of metabotropic glutamate receptor subtype 5 (mGlu5 receptor). Of the two geometric isomers of ABP688, (E)- ABP688 has a greater affinity towards mGlu5 receptors than (Z)-ABP688. Therefore, a high ratio of E-isomer is required when using [11C]ABP688 as a PET probe for imaging and quantification of mGlu5 receptors. The aim of this study was to evaluate the effect (Z)-[11C]ABP688 on the synthesis of [11C]ABP688 to be used for binding (E)-[11C]ABP688 in the brain. Methods: We synthesized and separated (E)- and (Z)-[11C]ABP688 by purification using an improved preparative high-performance liquid chromatography (HPLC) method equipped with a COSMOSIL Cholester column. We performed an in vitro binding assay in rat brain homogenates and PET studies of the rat brains using (E)- and (Z)-[11C]ABP688. Results: (E)- and (Z)-[11C]ABP688 were successfully obtained with suitable radioactivity for application. In the in vitro assay, the Kd value of (E)-[11C]ABP688 (5.7 nmol/L) was higher than that of (Z)-[11C]ABP688 (140 nmol/L). In the PET study of the rat brain, high radioactivity after injection of (E)-[11C]ABP688 was observed in regions rich in mGlu5 receptors such as the striatum and hippocampus. In contrast, after injection of (Z)-[11C] ABP688, radioactivity did not accumulate in the brain. Furthermore, BPND in the striatum and hippocampus was highly correlated (R2=0.99) with the percentage of (E)-[11C]ABP688 of the total radioactivity of (E)- and (Z)-[11C]ABP688 in the injection. Conclusion: We demonstrated that including (Z)-[11C]ABP688 in the [11C]ABP688 injection can decrease BPND in regions rich in mGlu5 receptors. Routine production of (E)-[11C]ABP688 will be helpful for imaging and quantification of mGlu5 receptors in clinical studies. |
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書誌情報 |
Nuclear Medicine and Biology 巻 41, 号 1, p. 17-23, 発行日 2013-09 |
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出版者 | ||||||
出版者 | ELSEVIER | |||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0969-8051 | |||||
DOI | ||||||
識別子タイプ | DOI | |||||
関連識別子 | doi.org/10.1016/j.nucmedbio.2013.09.008 |