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

doi:10.7538/tws.2014.27.04.0223

同位素 ›› 2014, Vol. 27 ›› Issue (4): 223-229.DOI: 10.7538/tws.2014.27.04.0223

• 放射性药物和标记化合物 • 上一篇下一篇

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¹;赵祚全^2,4;陈淑婷²;马云川¹;张现忠³;陆洁²

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.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；4.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

出版日期:2014-11-20 发布日期:2014-12-22

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

PENG Cheng¹;ZHAO Zuo-quan^2,4;CHEN Shu-ting²;MA Yun-chuan¹;ZHANG Xian-zhong³;LU Jie²

1.PET Center of Xuanwu Hospital, Capital Medical University, Beijing 10053, China; 2.Key Laboratory of Radiopharmaceuticals(Beijing Normal University), Ministry of Education,College of Chemistry, Beijing Normal University, Beijing 100875, China;3.Center for Molecular Imaging and Translational Medicine, State Key Laboratory of Molecular Vaccinology and Molecular Diagnostics, School of Public Health, Xiamen University, Xiamen 361102, China;4.Department of Nuclear Medicine, Cardiovascular Institute and FuWai Hospital, Chinese Academy of Medical Sciences, Beijing 100037, China

Online:2014-11-20 Published:2014-12-22

摘要/Abstract

摘要：

为研制新型的PET心肌灌注显像剂，设计合成了¹⁸F标记的鏻正阳离子：3-氟-¹⁸F-甲基苄基-三-（2,6-二甲氧基苯基）鏻盐（¹⁸F-2），并进行了小鼠生物分布研究。¹⁸F-2采用一锅法制备得到，总的标记时间小于60 min，校正后的产率为(31±3)%，放化纯度>95%；小鼠生物分布结果表明，¹⁸F-2在小鼠心肌中有很高的初始摄取和良好的滞留，给药后2 min和60 min的心肌摄取分别为(53.88±7.45)%ID/g和(23.93±3.28)%ID/g；其在肝、肺、血等非靶组织中的摄取低，且清除快，给药后60 min心与肝、心与肺、心与血放射性摄取比分别为3.99、3.80和9.17。值得进一步深入研究。

关键词: ¹⁸F标记, 鏻正阳离子, 心肌灌注显像剂

Abstract:

In order to develop new PET myocardial perfusion imaging agent, a novel ¹⁸F labeled phosphonium cation: (3-(［¹⁸F］fluoromethyl)benzyl) tris (2, 6-dimethoxyphenyl) phosphonium salt, ¹⁸F-2, had been designed and prepared. Biological evaluation of ¹⁸F-2 had been performed in Kunming normal mice. ¹⁸F-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 ¹⁸F-2 displayed a high heart uptake and good retention. The heart uptake of ¹⁸F-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 ¹⁸F-2 could be as a promising myocardial perfusion imaging agent for PET imaging.

Key words: ¹⁸F-labeled, phosphonium cation, myocardial perfusion imaging agent

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, 27(4): 223-229.

PENG Cheng;ZHAO Zuo-quan;CHEN Shu-ting;MA Yun-chuan;ZHANG Xian-zhong;LU Jie. Preparation and Biological Evaluation of Novel ¹⁸F-labeled Phosphonuim Cation for Myocardial Perfusion Imaging with PET[J]. Journal of Isotopes, 2014, 27(4): 223-229.

参考文献

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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

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

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