CAJ | 학술논문

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（18 F‐2），并进行了小鼠生物分布研究。18 F‐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，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。
위연제신형적PET심기관주현상제，설계합성료18 F표기적린정양리자：3‐불‐18 F‐갑기변기‐삼‐（2，6‐이갑양기분기）린염（18 F‐2），병진행료소서생물분포연구。18 F‐2채용일과법제비득도，총적표기시간소우60 min ，교정후적산솔위（31±3）％，방화순도＞95％；소서생물분포결과표명，18 F‐2재소서심기중유흔고적초시섭취화량호적체류，급약후2 min화60 min적심기섭취분별위（53.88±7.45）％ ID／g화（23.93±3.28）％ ID／g ；기재간、폐、혈등비파조직중적섭취저，차청제쾌，급약후60 min심여간、심여폐、심여혈방사성섭취비분별위3.99、3.80화9.17。치득진일보심입연구。
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 .