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Developing 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N- 11C-methylbenzamide for imaging of metabotropic glutamate 1 receptor in melanoma
https://repo.qst.go.jp/records/65682
https://repo.qst.go.jp/records/656822f671253-0fee-4667-8dd7-c5293f5e7dea
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2015-06-17 | |||||
| タイトル | ||||||
| タイトル | Developing 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N- 11C-methylbenzamide for imaging of metabotropic glutamate 1 receptor in melanoma | |||||
| 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_c94f | |||||
| 資源タイプ | conference object | |||||
| 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 |
Xie, Lin
× Xie, Lin× Fujinaga, Masayuki× Yamasaki, Tomoteru× Yui, Joji× Shimoda, Yoko× Hatori, Akiko× Kumata, Katsushi× Zhang, Yiding× Nengaki, Nobuki× Kawamura, Kazunori× Zhang, Ming-Rong× 謝 琳× 藤永 雅之× 山崎 友照× 由井 譲二× 下田 陽子× 羽鳥 晶子× 熊田 勝志× 張 一鼎× 念垣 信樹× 河村 和紀× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: Overexpression of metabotropic glutamate1 receptor (mGlu1) is found in brain and various cancers (1). Recently, we constructed the first mGlu1 oncoprotein-based PET platform with mGlu1-specific radioprobe 18F-FITM (2). However, 18F-FITM displayed high uptake of radioactivity both in brain and melanoma, which increased the risk of radiation-induced brain injury, then hampered its clinical application. In this study, using FITM as a lead compound, we developed a novel PET probe 4-iodo-N-[4-[6-(isopropylamino)pyrimidin-4-yl]-1,3-thiazol-2-yl]-N-11C-methyl- benzamide (11C-IITM) and explored its potential for melanoma imaging. Methods: 11C-IITM was synthesized by N-11C-methylation of the desmethyl precursor with 11C-CH3OTf. In vitro binding affinity for mGlu1 was assayed. PET imaging and biodistribution were performed in the mice bearing B16F10 melanoma with rich mGlu1 expression. Results: 11C-IITM was obtained with radiochemical yields of 20 5% (n > 10 based on 11C-CO2, EOS), radiochemical purity of >97%, and specific activity of 65–160 GBq/mol. PET showed high accumulation of radioactivity in target tumor (4.0 % ID/g) and very low uptake in non-target brain (0.9 % ID/g) in B16F10-bearing mice at 75 min after 11C-IITM injection. Ex vivo biodistribution confirmed the PET images and indicated better uptake ratio of tumor to brain in 11C-IITM (8.03 ± 0.46), compared with 18F-FITM (0.58 ± 0.05) at 90 min. In addition, the ratios of radioactivity for 11C-IITM in the tumor compared to blood, skin, and muscle at 90 min were 5-10. Treatment with an mGlu1 selective ligand significantly reduced radioactive uptake in the tumor. Conclusions: 11C-IITM is a useful PET tracer for mGlu1 imaging in melanoma. This radioprobe can be further developed by 124I and 131I labeling for long-duration PET scan and radiotherapeutic usage. |
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| 会議概要（会議名, 開催地, 会期, 主催者等） | ||||||
| 内容記述タイプ | Other | |||||
| 内容記述 | SNMMI 2015 Annual Meeting | |||||
| 発表年月日 | ||||||
| 日付 | 2015-06-10 | |||||
| 日付タイプ | Issued | |||||
