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Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography
https://repo.qst.go.jp/records/44941
https://repo.qst.go.jp/records/449417c4b77ad-81fe-4069-83d6-088d496ddacd
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2007-08-15 | |||||
| タイトル | ||||||
| タイトル | Synthesis and evaluation of fluorine-18-labeled SA4503 as a selective sigma1 receptor ligand for positron emission tomography | |||||
| 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× Tsukada, Hideo× Shiba, Kazuhiro× Kimura, Yuichi× Ishiwata, Kiichi× et.al× 木村 裕一× 石渡 喜一 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The [18F]fluoromethyl analog of the sigma1 selective ligand 1-(3,4-dimethoxyphenethyl)-4-(3-phenylpropyl)piperazine dihydrochloride (SA4503) ([18F]FM-SA4503) was prepared and its potential evaluated for the in vivo measurement of sigma1 receptors with positron emission tomography (PET). FM-SA4503 had selective affinity for the sigma1 receptor (Ki for sigma1 receptor, 6.4 nM; Ki for sigma2 receptor, 250 nM) that was compatible with the affinity of SA4503 (Ki for sigma1 receptor, 4.4 nM; Ki for sigma2 receptor, 242 nM). [18F]FM-SA4503 was synthesized by 18F-fluoromethylation of O-demethyl SA4503 in the radiochemical yield of 2.9-16.6% at the end of bombardment with a specific activity of 37.8-283 TBq/mmol at the end of synthesis. In mice, the uptake of [18F]FM-SA4503 in the brain was gradually increased for 30 min after injection, and then decreased. In the blocking study, brain uptake was significantly decreased by co-injection of haloperidol to 32% of control, and FM-SA4503 to 52% of control. In PET study of the monkey brain, high uptake was found in the cerebral cortex, thalamus and striatum. The radioactivity level of [18F]FM-SA4503 in the brain regions gradually increased over a period of 120 min after injection, followed by a stable plateau phase until 180 min after injection. In pretreatment with haloperidol measurement of the monkey brain, the radioactivity level was 22-32% and 11-25% of the baseline at 60 and 180 min, respectively, after injection, suggesting high receptor-specific binding. [18F]FM-SA4503 showed specific binding to sigma1 receptors in mice and monkeys; therefore, [18F]FM-SA4503 has the potential for mapping sigma1 receptors in the brain. | |||||
| 書誌情報 |
Nuclear Medicine and Biology 巻 34, 号 5, p. 571-577, 発行日 2007-05 |
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| 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 | 10.1016/j.nucmedbio.2007.03.009 | |||||
