1-(3'-〔125I〕iodophenyl)-3-methy-2-pyrazolin-5-one: preparation, solution stability, and biodistribution in normal mice
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- Sano Yuuhei
- Graduate School of Pharmaceutical Sciences, Kyushu University
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- Motomura Tomokazu
- Graduate School of Pharmaceutical Sciences, Kyushu University
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- Yamamoto Fumihiko
- Graduate School of Pharmaceutical Sciences, Kyushu University
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- Fukuda Miki
- Graduate School of Pharmaceutical Sciences, Kyushu University
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- Mukai Takahiro
- Graduate School of Pharmaceutical Sciences, Kyushu University
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- Maeda Minoru
- Graduate School of Pharmaceutical Sciences, Kyushu University
書誌事項
- タイトル別名
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- 1-(3'-[125I]Iodophenyl)-3-methy-2-pyrazolin-5-one: Preparation, Solution Stability, and Biodistribution in Normal Mice
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抄録
3-Methyl-1-phenyl-2-pyrazolin-5-one (edaravone, 1), known as a potent free radical scavenger, has been developed as a medical drug for the treatment of acute cerebral infarction. With the aim of developing radiotracers for imaging free radicals in vivo, 1-(3′-[125I]iodophenyl)-3-methy-2-pyrazolin-5-one (125I-2) was synthesized by two methods, via isotopic exchange and interhalogen exchange under solvent-free conditions, in which iodo- and bromo-derivatives were used as labeling precursors, respectively. After HPLC purification, 125I-2 was obtained in modest isolated radiochemical yields (ca. 20%) with high radiochemical purities by both methods. The former gave specific activities of 0.2—0.6 kBq/μmol, whereas the latter approach achieved specific activities of more than 0.14 GBq/μmol. On attempting to prepare an injectable formulation for 125I-2 with high specific activity, its radiochemical purities dropped to about 60—70%. Unlabeled analog 2 was found to have lipophilic and antioxidant properties similar to edaravone. Intravenous injection of 125I-2 with low specific radioactivity into normal mice showed signs of distribution profiles similar to reported results for 14C-labeled edaravone in normal rats.
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 58 (8), 1020-1025, 2010
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679149830656
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- NII論文ID
- 130000299808
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 10764009
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
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