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Synthesis of Two Novel [18F]Fluorobenzene-Containing Radiotracers via Spirocyclic Iodonium Ylides and Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic Brain
https://repo.qst.go.jp/records/49257
https://repo.qst.go.jp/records/492574c98d5e8-cf45-4dd3-a67c-96c1c4c4db9d
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-09-03 | |||||
| タイトル | ||||||
| タイトル | Synthesis of Two Novel [18F]Fluorobenzene-Containing Radiotracers via Spirocyclic Iodonium Ylides and Positron Emission Tomography Imaging of Translocator Protein (18 kDa) in Ischemic 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 |
Fujinaga, Masayuki
× Fujinaga, Masayuki× Kumata, Katsushi× Zhang, Yiding× Hatori, Akiko× Yamasaki, Tomoteru× Mori, Wakana× Ohkubo, Takayuki× Xie, Lin× Nengaki, Nobuki× Ming-Rong, Zhang× Fujinaga, Masayuki× Kumata, Katsushi× Zhang, Yiding× Hatori, Akiko× Yamasaki, Tomoteru× Mori, Wakana× Ohkubo, Takayuki× Xie, Lin× Nengaki, Nobuki× Ming-Rong, Zhang |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | Two novel radiotracers, namely, N-(4-[18F]fluorobenzyl) -N-methyl-2-(7-methyl-8-oxo-2-phenyl-7,8-dihydro-9H-purin-9-yl)acetamide ([18F]5) and 2-(5-(4-[18F]fluorophenyl)-2-oxobenzo[d]oxazol-3(2H)-yl)-N-methyl-N-phenylacetamide ([18F]6), were developed for positron emission tomography (PET) imaging of translocator protein (18 kDa) (TSPO) in ischemic brain in this study. The two radiotracers with a [18F]fluorobenzene ring were derived from the corresponding [18F]fluoroethyl tracers [18F]7 and [18F]8 which underwent [18F]defluoroethylation in vivo easily. [18F]5 or [18F]6 was synthesized by the radiofluorination of the spirocyclic iodonium ylide precursor 10 or 17 with [18F]F- in 23 ± 10 % (n = 7) or 56 ± 9% (n = 7) radiochemical yields (decay-corrected, based on [18F]F-). [18F]5 and [18F]6 showed high in vitro binding affinities (Ki = 0.70 nM and 5.9 nM) for TSPO and moderate lipophilicities (LogD = 2.9 and 3.4). Low uptake of radioactivity for both radiotracers was observed in mouse bones. Metabolite analysis showed that the in vivo stability of [18F]5 and [18F]6 was improved in comparison to the parent radiotracer [18F]7 and [18F]8. In particular, no radiolabelled metabolite of [18F]5 was found in the mouse brains at 60 min after the radiotracer injection. PET studies with [18F]5 on ischemic rat brains revealed a higher binding potential (BPND = 3.42) and maximum uptake ratio (4.49) between the ipsilateral and contralateral sides. Thus, [18F]5 was shown to be a useful PET radiotracer for visualizing TSPO in neuroinflammation models. | |||||
| 書誌情報 |
Organic & Biomolecular Chemistry 巻 2018, 号 16, p. 8325-8335, 発行日 2018-08 |
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| 出版者 | ||||||
| 出版者 | Royal Society of Science | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 1477-0520 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1039/C8OB01700J | |||||
