^(18)F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

作　　者：彭程[1] 赵祚全[2,3] 陈淑婷[2] 马云川[1] 张现忠[4] 陆洁[2] 

机构地区：[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

出　　处：《同位素》2014年第4期223-229,共7页Journal of Isotopes

基　　金：国家自然科学基金项目(20871020;21271030;81471707)

摘　　要：为研制新型的PET心肌灌注显像剂,设计合成了18 F标记的鏻正阳离子:3-氟-18 F-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60min,校正后的产率为(31±3)%,放化纯度>95%;小鼠生物分布结果表明,18 F-2在小鼠心肌中有很高的初始摄取和良好的滞留,给药后2min和60min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60min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。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＆amp;nbsp;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 

分 类 号：O615.4[理学—无机化学]