^(99m)Tc-RET的制备及其在正常小鼠体内分布和药代动力学研究  

Biodistribution Characteristics and Pharmacokinetics in Nomal Mice and Uptake in Human Lung Cancer Cells of ^(99m)Tc-RET

作　　者：谢文晖[1] 章斌[2] 刘慈懿[1] 常城[1] 雷贝[1] 王利华[1] 吴翼伟[2] 

机构地区：[1]上海交通大学附属胸科医院核医学科,上海200030 [2]苏州大学附属第一医院核医学科,苏州215006

出　　处：《中国医药导刊》2014年第10期1339-1342,共4页Chinese Journal of Medicinal Guide

基　　金：上海市卫生局项目(项目编号:2010066);上海市科委自然基金项目(项目编号:11ZR1433700)资助

摘　　要：目的:研究99mTc-RET(Arg-Glu-Thr)与肺癌细胞结合及其在正常小鼠体内分布和药代动力学。方法:采用99mTc直接法标记RET,行99mTc-RET与非小细胞肺癌细胞A549和H1299的结合实验。正常小鼠尾静脉注射99mTc-RET后不同时间处死,取主要脏器或组织,测定其每克组织百分注射剂量率(%ID/g)。另取尾静脉注射99mTc-RET后不同时间小鼠血液,测量放射性计数并计算药代动力学参数。结果:99mTc直接标记RET的标记率大于90%。99mTc-RET与非小细胞肺癌细胞A549和H1299的最高特异性结合率分别为(3.78±0.29)%和(3.56±0.37)%。体内分布提示99mTc-RET在小鼠血液中清除迅速,2h时放射性仅为注射5min时的26%,肝脏内放射性浓聚较多,且呈缓慢下降,肾脏、心、肺放射性摄取随时间逐渐下降,其余组织放射性呈低水平。结论:99mTcm-RET具有亲肺癌细胞的特性,有可能成为一种亲肺癌肿瘤显像剂。Objective： To investigate the biodistribution characteristics and pharmacokinetics in nomal mice and uptake in human lung cancer cells of99mTc labeled arginine-glutamic-glutamic（RET）.Methods：RET was labeled directly with99mTc The biodistribution of99mTc-RET was studied at 2min,5 min,10min,30min,1h,2h,4h,8h,and 24h,respectively,after intravenous injection in normal mice. At different time points,the mice were sacrificed and organs of interest were excised,weighted and counted by a gamma counter. The organ uptake was calculated as a %ID/g.Results：The radiochemical purity of 99mTc-RET were more than 90%,and the specific binding efficiency of 99mTc-RET with A549 and H1299 cells was （3.78±0.29）% and （3.56±0.37）%. In the first 24h after injection,the biodistribution in mice showed rapid blood excretion and most of the radioactivity was observed in liver.Conclusion：99mTc-RET can be uptaked in human lung cancer cells,and might possibly become a potential lung cancer imaging agent.

关 键 词：多肽 锝 肺癌 药代动力学 精氨酸-谷氨酸-苏氨酸 

分 类 号：R969.1[医药卫生—药理学]