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PET study using [ 11C]FTIMD with ultra-high specific activity to evaluate I2-imidazoline receptors binding in rat brains
https://repo.qst.go.jp/records/46286
https://repo.qst.go.jp/records/462866d755cf7-c46a-49d3-b3a1-b9723e0fa7bf
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2012-03-19 | |||||
| タイトル | ||||||
| タイトル | PET study using [ 11C]FTIMD with ultra-high specific activity to evaluate I2-imidazoline receptors binding in rat brains | |||||
| 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× Kimura, Yuichi× Yui, Joji× Wakizaka, Hidekatsu× Yamasaki, Tomoteru× Hatori, Akiko× Kumata, Katsushi× Fujinaga, Masayuki× Yoshida, Yuichirou× Ogawa, Masanao× Nengaki, Nobuki× Fukumura, Toshimitsu× Zhang, Ming-Rong× 河村 和紀× 木村 裕一× 由井 譲二× 脇坂 秀克× 山崎 友照× 羽鳥 晶子× 熊田 勝志× 藤永 雅之× 吉田 勇一郎× 小川 政直× 念垣 信樹× 福村 利光× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Introduction: We recently developed a selective 11C-labeled I2-imidazoline receptor (I2R) ligand, 2-(3-fluoro-4-[11C]tolyl)-4,5-dihydro-1H-imidazole ([11C]FTIMD). [11C]FTIMD showed specific binding to I2Rs in rat brains having a high density of I2R, as well as to I2Rs those in monkey brains, as illustrated by positron emission tomography (PET) and autoradiography. However, [11C]FTIMD also showed moderate non-specific binding in rat brains. In order to increase the specificity for I2R in rat brains, we synthesized [11C]FTIMD with ultra-high specific activity and evaluated its binding. Methods: [11C]FTIMD with ultra-high specific activity was prepared by a palladium-promoted cross-coupling reaction of the tributylstannyl precursor and [11C]methyl iodide, which was produced by iodination of [11C]methane using the single-pass method. Dynamic PET scans were conducted in rats, and the kinetic parameters were estimated. Results: [11C]FTIMD with ultra-high specific activity was successfully synthesized with an appropriate level of radioactivity and ultra-high specific activity (4470+/-1660 GBq/mumol at end of synthesis, n=11) for injection. In the PET study, distribution volume (VT) values in all the brain regions investigated whether I2R expression was greatly reduced in BU224-pretreatead rats compared with control rats (29–45% decrease). Differences in VT values between control and BU224-pretreated rats using [11C]FTIMD with ultra-high specific activity were greater than those using [11C]FTIMD with normal specific activity (17–34% decrease) in all brain regions investigated. Conclusion: Quantitative PET using [11C]FTIMD with ultra-high specific activity can contribute to the detection of small changes in I2R expression in the brain. |
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| 書誌情報 |
Nuclear Medicine and Biology 巻 39, 号 2, p. 199-206, 発行日 2012-02 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0969-8051 | |||||
