^(11)C标记石杉碱甲的制备及其在动物体内的生物学分布  

Synthesis and biodistribution in animals of ^(11)C-huperzine A

作　　者：闫瑾[1] 管一晖[2] 薛方平[2] 张政伟[2] 刘平[2] 林祥通[2] 

机构地区：[1]河南省肿瘤医院PET-CT中心,郑州450008 [2]复旦大学附属华山医院PET中心,上海200235

出　　处：《郑州大学学报（医学版）》2010年第5期767-769,共3页Journal of Zhengzhou University(Medical Sciences)

基　　金：国家卫生部核医学重点实验室基金资助项目WK006002

摘　　要：目的:研究11C标记石杉碱甲(HupA)的制备方法及其在大鼠体内的生物学分布。方法:由美国CTI公司RDS111加速器生产11C-CO2,用碘代甲烷模块将11C-CO2转化成11C-碘代甲烷,再转化为11C-三氟甲基磺酰甲烷后传入到11C-HupA前体的乙醇溶液中,在常温下反应得到产物。SD大鼠静脉给药后不同时间处死,分别取不同器官称量并测定放射性计数。结果:11C-HupA放化合成时间为10～20min,放化纯度大于98%,比活度47.4GBq/mmol,放化产物相对分子质量为257,稳定性检测2h内放化纯度>90%,11C-HupA注射液在室温条件下放置5、15、30、60、90和120min的放化纯度分别为98.2%、97.8%、96.2%、95.7%、93.2%和91.6%。主要质量控制指标达到正电子放射性药物质量要求。11C-HupA进入大鼠体内具有血液清除快的特点,经肝胆系统代谢,肾脏是11C-HupA的主要排泄器官。在大脑皮层、海马、丘脑及脑干分布较多。结论:合成的11C-HupA注射液符合进一步的动物或人体探索性研究要求。Aim：To research the method of 11C-radiolabeled HupA synthesis and explore its biodistribution in vivo.Methods：11CO2 was produced by CTI RDS 111 accelerator,and converted to 11C-CH3I by CH3I die-block,and then converted it to 11C-Triflate-CH4,imported 11C-Triflate-CH4 to Hup A which was dissolved in alocohol,reacted at common temperature and then obtained the product.The SD rats were sacrificed,brain and tissue samples from other organs were weighed and radiocounted.Results：The synthesis time of 11C-HupA was 10 to 20 min with radiochemical purity 98%,and average specific activity of 47.4 GBq/mmol,the molecular weight of labeled product was 257,radiochemical purity 90% in 2 hours.The RCP of 11C-HupA in 5,15,30,60,90 and 120 min was 98.2%,97.8%,96.2%,95.7%,93.2% and 91.6% respectively.All quality criteria of 11C-HupA met the requirements of the positron radio-pharmaceuticals.11C-HupA was of the characteristic that quickly discharge from the blood,metabolism through the liver,kidney was the main eccrisis organ,and there were more distribution in cerebral cortex,hippocampus,cerebral ganglion and brain stem.Conclusion：11C-HupA injections can be used to further study in the animal or human study.

关 键 词：石杉碱甲 放射性同位素 生物学分布 

分 类 号：R817.4[医药卫生—影像医学与核医学]