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Development of [18F] ethyl fluoroacetate as a tracer of oxidative metabolism in the brain
https://repo.qst.go.jp/records/71217
https://repo.qst.go.jp/records/7121738903dae-c147-4713-b3e1-412c1fe9efa4
| Item type | 会議発表用資料 / Presentation(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2013-08-29 | |||||
| タイトル | ||||||
| タイトル | Development of [18F] ethyl fluoroacetate as a tracer of oxidative metabolism in the 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_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 |
Mori, Tetsuya
× Mori, Tetsuya× Kobayashi, Masakazu× Kiyono, Yashushi× Furukawa, Takako× Fujibayashi, Yasuhisa× et.al× 古川 高子× 藤林 康久 |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Objectives: F-18 labeled fluoroacetate (FA) has been developed as a PET tracer for imaging of oxidative metabolism in various tissues. For brain studies, however, the low blood-brain barrier (BBB) permeability of anionic form like FA is a fundamental problem. It is well known that ethyl acetate penetrates easily into the brain, then, is hydrolyzed to acetate rapidly in vivo. Based on these characteristics, we selected F-18 labeled ethyl fluoroacetate (EFA), ethyl-ester of FA, as a potential candidate for PET tracer of oxidative metabolism in brain. In this study, we investigated the possibility of [18F] EFA for brain PET imaging. Methods: BBB permeability was estimated by brain uptake index (BUI) method. Stability of [14C] EFA in plasma was assessed using five animal species. Then, the ester hydrolysis rate in rat brain was assayed both in vitro and in vivo. After these preliminary studies, we performed PET and metabolism studies of [18F] EFA using non-human primates. Results: The BUI of [14C] EFA was 125.9 +- 4.1% (n=4). This value was much higher than [14C] FA and also higher than that of [3H] H2O. The stability studies in plasma showed that [14C] EFA was extremely unstable in rodent, but stable in primate. Dog plasma brought an intermediate rate of degradation. The [14C] EFA was hydrolyzed rapidly in rat brain. These results suggest that EFA can be used as a pro-drug of [18F] FA for cerebral PET studies and the primate is suitable for in vivo experiments. In PET study using common marmosets, [18F] EFA showed higher brain uptake compared to [18F] FA at initial period, and the radioactivity was retained at 90 min after injection. The metabolism studies revealed that [18F] EFA was metabolized to only [18F] FA in arterial blood at 60 min after injection, but was converted to [18F] fluorocitrate in the brain, an intermediate metabolite from FA in the TCA cycle. Conclusions: we confirmed that [18F] EFA has ideal characteristics for brain imaging and it is a possible. |
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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 | Society of nuclear medicine 54rd Annual Meetng | |||||
| 発表年月日 | ||||||
| 日付 | 2007-06-06 | |||||
| 日付タイプ | Issued | |||||
