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18F标记的新型鏻正阳离子 PET 心肌灌注显像剂的制备及生物性能评价

彭程 赵祚全 陈淑婷 马云川 张现忠 陆洁

同位素Issue(4):223-229,7.
同位素Issue(4):223-229,7.DOI:10.7538/tws.2014.27.04.0223

18F标记的新型鏻正阳离子 PET 心肌灌注显像剂的制备及生物性能评价

Preparation and Biological Evaluation of Novel 18 F-labeled Phosphonuim Cation for Myocardial Perfusion Imaging with PET

彭程 1赵祚全 2陈淑婷 3马云川 2张现忠 1陆洁4

作者信息

  • 1. 首都医科大学宣武医院,北京 100053
  • 2. 放射性药物教育部重点实验室北京师范大学化学学院,北京 100875
  • 3. 中国医学科学院北京协和医学院国家心血管病中心阜外心血管病医院心血管疾病国家重点实验室,北京 100037
  • 4. 分子影像暨转化医学研究中心厦门大学公共卫生学院,厦门 361005
  • 折叠

摘要

Abstract

In order to develop new PET myocardial perfusion imaging agent ,a novel 18 F labeled phosphonium cation :(3‐([18 F]fluoromethyl)benzyl) tris (2 ,6‐dimethoxyphe‐nyl) phosphonium salt ,18 F‐2 ,had been designed and prepared .Biological evaluation of 18 F‐2 had been performed in Kunming normal mice .18 F‐2 was obtained by a simple one‐pot method and the radiochemical yield was (31 ± 3)% .The total radio‐synthesis time was less than 60 min and the radiochemical purity of final radiotracer was more than 95% .The biodistribution of 18 F‐2 displayed a high heart uptake and good retention . The heart uptake of 18 F‐2 at 5 and 60 min post‐injection were (53.88 ± 7.45)% ID/g and (23.93 ± 3.28)% ID/g ,respectively .18F‐2 exhibited low radio‐accumulation in non‐target tissues and rapid clearance in liver ,lung and blood .The heart to liver ,heart to lungs and heart to blood ratio values were 3.99 ,3.80 and 9.17 ,respectively .The results indicated that 18 F‐2 could be as a promising myocardial perfusion imaging agent for PET imaging .

关键词

18F标记/鏻正阳离子/心肌灌注显像剂

Key words

18 F labeled/phosphonium cation/myocardial perfusion imaging agent

分类

化学化工

引用本文复制引用

彭程,赵祚全,陈淑婷,马云川,张现忠,陆洁..18F标记的新型鏻正阳离子 PET 心肌灌注显像剂的制备及生物性能评价[J].同位素,2014,(4):223-229,7.

基金项目

国家自然科学基金项目 ()

同位素

OACSTPCD

1000-7512

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