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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) | |||||
|---|---|---|---|---|---|---|
| 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 | |||||
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| 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 | |||||
