| 细胞凋亡显像剂18F-ML-8的合成及显像研究 |
| 投稿时间：2015-11-11 修订日期：2015-12-07 点此下载全文 |
| 引用本文：要少波,唐刚华,蔡炯,霍力,姜申德,李方.细胞凋亡显像剂18F-ML-8的合成及显像研究[J].医学研究杂志,2016,45(7):25-29,43 |
| DOI：
10.11969/j.issn.1673-548X.2016.07.008 |
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| 基金项目:国家自然科学基金资助项目（81571712） |
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| 中文摘要: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18F-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18F离子计算合成18F-ML-8需要25min，放化收率为55%±4%（n=10），结果未经衰变矫正，18F-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18F-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。 |
| 中文关键词:自动化合成|18F-ML-8|细胞凋亡|PET |
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| Radiosynthesis of a Novel Apoptosis-imaging Probe18F-ML-8 and Its PET Study |
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| Abstract:Objective To evaluate the importance of side chain length to the 18F-ML-10, a novel compound with two carbon shorter and improved lipophilicity was designed and synthesized. Methods The automated radiosynthesis was finished in two simple steps including nucleophilic 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 18F-ML-8 was obtained with yield 55%±4% (n=10, decay-uncorrected) based on 18F ion within 25 min. The radiochemical purity of 18F-ML-8 was no less than 99% and the specific activity was greater than 38.5%±11.2GBq/μmol (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 radiotracer used for clinical and scientific study with positron emission tomography (PET) imaging. |
| keywords:Automated synthesis|18F-ML-8|Apoptosis|PET |
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