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

  • 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。

     

    Abstract: In order to develop new PET myocardial perfusion imaging agent, a novel 18F labeled phosphonium cation: (3-(18Ffluoromethyl)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.

     

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