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18F-FEAC and 18F-FEDAC : PET of the Monkey Brain and Imaging of Translocator Protein (18 kDa) in the Infarcted Rat Brain
https://repo.qst.go.jp/records/45873
https://repo.qst.go.jp/records/4587381ffd4ad-307b-411e-a841-0eb0a7fff75e
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2010-08-03 | |||||
| タイトル | ||||||
| タイトル | 18F-FEAC and 18F-FEDAC : PET of the Monkey Brain and Imaging of Translocator Protein (18 kDa) in the Infarcted Rat Brain | |||||
| 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 |
Yui, Joji
× Yui, Joji× Maeda, Jun× Kumata, Katsushi× Kawamura, Kazunori× Yanamoto, Kazuhiko× Hatori, Akiko× Yamasaki, Tomoteru× Nengaki, Nobuki× Higuchi, Makoto× Zhang, Ming-Rong× 由井 譲二× 前田 純× 熊田 勝志× 河村 和紀× 柳本 和彦× 羽鳥 晶子× 山崎 友照× 念垣 信樹× 樋口 真人× 張 明栄 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | We evaluated two 18F-labeled PET ligands, N-benzyl-N-ethyl-2-[7,8-dihydro-7-(2-18F-fluoroethyl)-8-oxo-2-phenyl-9H-purin-9-yl]acetamide (18F-FEAC) and N-benzyl-N-methyl-2-[7,8-dihydro-7-(2-18F-fluoroethyl)-8-oxo-2-phenyl-9H-purin-9-yl]acetamide (18F-FEDAC), by investigating their kinetics in the monkey brain and by performing in vitro and in vivo imaging of translocator protein (18 kDa) (TSPO) in the infarcted rat brain. Methods: Dissection was used to determine the distribution of 18F-FEAC and 18F-FEDAC in mice, whereas PET was used for a monkey. With each 18F-ligand, in vitro autoradiography and small-animal PET were performed on infarcted rat brains. Results: 18F-FEAC and 18F-FEDAC had a high uptake of radioactivity in the heart, lung, and other TSPO-rich organs of mice. In vitro autoradiography showed that the binding of each 18F-ligand significantly increased on the ipsilateral side of rat brains, compared with the contralateral side. In a small-animal PET study, PET summation images showed the contrast of radioactivity between ipsilateral and contralateral sides. Pretreatment with TSPO ligands N-benzyl-N-ethyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide (AC-5216) or (R)-N-methyl-N-(1-methylpropyl)-1-(2-chlorophenyl)isoquinoline-3-carboxamide (PK11195) diminished the difference in uptake between the 2 sides. The PET study showed that each 18F-ligand had uptake and distribution patterns in the monkey brain similar to those of 11C-AC-5216. After injection into the monkey during PET, the uptake of each 18F-ligand in the brain decreased over time whereas 11C-AC-5216 did not. In the brain homogenate of mice, the percentage of the fraction corresponding to intact 18F-FEAC and 18F-FEDAC was 68% and 75% at 30 min after injection. In monkey plasma, each 18F-ligand was scarcely metabolized until the end of the PET scan. Conclusion: 18F-FEAC and 18F-FEDAC produced in vitro and in vivo signals allowing visualization of the increase in TSPO expression in the infarcted rat brain. The kinetics of both 18F-ligands in the monkey brain and tolerance for in vivo metabolism suggested their usefulness for imaging studies of TSPO in primates. | |||||
| 書誌情報 |
Journal of Nuclear Medicine 巻 51, 号 8, p. 1301-1309, 発行日 2010-08 |
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| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0161-5505 | |||||
