细胞凋亡显像剂^(18)F-ML-8的合成及显像研究  

Radiosynthesis of a Novel Apoptosis-imaging Probe ^(18)F-ML-8 and Its PET Study

作　　者：要少波[1] 唐刚华[2] 蔡炯[1] 霍力[1] 姜申德[3] 李方[1] 

机构地区：[1]中国医学科学院北京协和医院核医学科,北京100730 [2]中山大学附属第一医院核医学科,广州510080 [3]天津大学药物科学与技术学院,300072

出　　处：《医学研究杂志》2016年第7期25-29,43,共6页Journal of Medical Research

基　　金：国家自然科学基金资助项目(81571712)

摘　　要：目的通过减少已报道凋亡显像剂ML-10侧链的长度提高分子的脂溶性,探索其放化标记的自动化合成过程及对显像作用的影响。方法使用国产PET-MF-2V-IT-I合成模块,通过亲核、碱水解两步简单的反应,即可得到^(18)F-ML-8,产物可以依次通过ICH-Al2O3-C18柱的达到纯化的目的,对氟化反应的温度和时间做了正交实验以确定最佳反应条件,并且还进行了相应的生物学实验初步评价。结果从^(18)F离子计算合成^(18)F-ML-8需要25min,放化收率为55%±4%(n=10),结果未经衰变矫正,^(18)F-ML-8注射液的放化纯度不小于99%,比活度为38.5±11.2GBq/μmol(n=10)。结论使用多功能合成模块完成"一锅法"自动化合成^(18)F-ML-8,操作简便,质控符合相关放药质量管理条例规定,可以满足临床显像的要求。Objective To evaluate the importance of side chain length to the 18F - ML - 10, a novel compound with two carbon shor- ter and improved lipophilicity was designed and synthesized. Methods The automated radiosynthesis was finished in two simple steps in- eluding nueleophilic substitution and base - catalyzed hydrolysis on a modified PET - MF - 2V - IT - I synthesizer. Orthogonal test was performed to confirm the suitable reaction conditions （temperature and time）. Also, some preclinical evaluation was performed. Results lS F - ML -8 was obtained with yield 55% ± 4% （n = 10, decay - uncorrected） based on 18F ion within 25 min. The radiochemieal purity of 18F - ML - 8 was no less than 99% and the specific activity was greater than 38.5% ± 11.2GBq/ixmol （n = 10）. Conclusion 18F - ML - 8 injection saline is easily to be prepared in ＂one - pot reaction＂ and good quality satisfying the quality control demand, it is a promising radiotraeer used for clinical and scientific study with positron emission tomography （PET） imaging.

关 键 词：自动化合成 18F-ML-8 细胞凋亡 PET 

分 类 号：R817.4[医药卫生—影像医学与核医学]