[1]袁志斌,冨吉勝美,樋口徹也,等.18F亲电反应法直接标记氨基酸衍生物的研究[J].国际放射医学核医学杂志,2006,30(2):69-72.
　YUAN Zhi-bin,TOMIYOSHI Katsumi,HIGUCHI Tetsuya,et al.Study on direct electrophilic radiofluorination of amino acid derivatives[J].International Journal of Radiation Medicine and Nuclear Medicine,2006,30(2):69-72.
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《国际放射医学核医学杂志》[ISSN:1673-4114/CN:12-1381/R]

卷:
30
期数:
2006年第2期
页码:
69-72
栏目:
实验核医学
出版日期:
1900-01-01

文章信息/Info

Title:
Study on direct electrophilic radiofluorination of amino acid derivatives
作者:
袁志斌1;  冨吉勝美2;  樋口徹也2;  織内昇2;  遠藤啓吾2
1. 200233 上海, 上海交通大学附属第六人民医院核医学科;
2. 371-8511 日本, 日本群马大学医学部核医学
Author(s):
YUAN Zhi-bin1;  TOMIYOSHI Katsumi2;  HIGUCHI Tetsuya2;  ORIUCHI Noboru2;  ENDO Keigo2
1. Department of Nuclear Medicine, Shanghai 6th People’s Hospital, Shanghai Jiao Tong University, Shanghai 200233, China;
2. Department of Nuclear Medicine, Gunma University School of Medicine, Maebashi 371-8511, Japan
关键词:
氨基酸; 氟放射性同位素; 同位素标记
Keywords:
Amino acid; Fluorine radioisotopes; Isotope labeling
分类号:
R817.9
摘要:
目的 用18F亲电反应法,研究一种方便、迅速的18F标记氨基酸衍生物的方法。方法 标记过程分三步进行:①加速器内20Ne (d,α)18F反应合成18F2气体;②18F2气体通过特制的反应柱,转化为CH3COO18F;③CH3COO18F与氨基酸衍生物直接反应,得到相应的标记物。结果 整个标记过程约为45min,放射性产额约60%,放射化学纯度>95%,pH值约为7,无菌性和热源实验均为阴性,这些结果保证了进一步动物实验和临床应用的可行性。结论 18F亲电反应法是一种简单易行的标记氨基酸衍生物的方法。
Abstract:
Objective To study an easy and fast method for the radiofluorination of amino acid derivatives.Methods The radiosynthesis procedure was divided into 3 steps:(1) Synthesis of 18F2gas by 20Ne (d,α)18F reaction in cyclotron. (2) By passing through a specific column, 18F2 gas was converted into CH3COO18F. (3) Fluorinated amino acid derivatives were synthesized by direct electrophilic reaction between amino acids and CH3COO18F.Results It took about 45 minutes to fulfill the whole synthesis procedure. The radioactivity yield rate, radiochemistry purity and pH value was about 60%, >95% and about 7 respectively. Both sterility and apyrogenicity test showed negative result. All these results guaranteed the following animal study and clinical application.Conclusion It is suggested that electrophilic radiofluorination reaction is an easy and fast way for the radiolabeling of amino acid derivatives.

参考文献/References:

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2 Ehrenkaufer RE,Potocki JF,Jewett DM,et al.Simple synthesis of F-18-1abeled 2-fluoro-2-deoxy-d-glucose:concise communication.J Nucl Med,1984,25(3):333-337.
3 Jager PL,Vaalburg W,Pruim J,et al.Radiolabled amino acids:basic aspects and clinical applications in oncology.J Nucl Med,2001,42(3):432-445.
4 Inoue T,Koyama K,Oriuchi N,et al.Detection of malignant tumors:whole-body PET with fluorine-18 alpha-methyl tyrosine versus 18F-FDG-prelimary study.Radiology,2001,220(1):54-62.
5 Kaasinen V,Nurmi E,Bruck A,et al.Increased frontal[18F]fluorodopa uptake in early Parkinson’s disease:sex differences in the prefrontal cortex.Brain,2001,124(6):1125-1130.
6 Hamacher K.Phase-transfer catalysed synthesis of 4-s-β-D-glucopyranosyl-4-thio-D-glucopyranose (Thiocellobiose)and 2-s-β-D-glu-copyranosyl-2-thio-D-glucopyranose (Thiosophorose).Carbohydrate Res,1984,128(2):291-295.

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备注/Memo

备注/Memo:
收稿日期:2005-09-20。
通讯作者:袁志斌(E-mail:yuanzb@sh163.net)
更新日期/Last Update: 1900-01-01