两个^(99)Tc^m标记胸苷衍生物在小鼠体内分布的比较  

Comparison of Biodistribution of Two ^(99)Tc^m-Labeled Thymidine Analogs in Mice

作　　者：陆春雄[1,2] 蒋泉福[1] 唐婕[1] 谭成[1] 张建康[1] 

机构地区：[1]江苏省原子医学研究所卫生部核医学重点实验室/江苏省分子核医学重点实验室,江苏无锡214063 [2]江南大学化学与材料工程学院,江苏无锡214122

出　　处：《核化学与放射化学》2011年第6期363-369,共7页Journal of Nuclear and Radiochemistry

基　　金：江苏省自然科学基金资助项目(BK2008112);江苏省卫生厅资助项目(H200624)

摘　　要：为了找到适合肿瘤显像的99 Tcm标记胸苷衍生物,制备了2个标记物99 Tcm-ANMdU和99 Tcm-NHT,标记率均大于95%,且稳定性好。生物分布结果显示:99 Tcm-ANMdU主要经肾脏代谢,在体内清除比较迅速;99 Tcm-ANMdU注射60min后,荷瘤鼠体内肿瘤的放射性摄取与肌肉、骨和血的放射性摄取的比值达到较高值,分别为1.58±0.17、1.95±0.31和1.17±0.08;99 Tcm-NHT在小鼠体内肝脏和肾脏的放射性摄取很高,说明其主要经肝脏和肾脏代谢,体内的清除相对较慢;99 Tcm-NHT注射120min后,荷瘤鼠体内肿瘤的放射性摄取与肌肉、骨和血的放射性摄取的比值达到较高值,分别为4.41±0.32、2.45±0.24和1.51±0.18。因此,99 Tcm-NHT虽然在体内清除比99 Tcm-ANMdU缓慢,但99 Tcm-NHT在肿瘤的放射性摄取相对较高,可能是潜在的SPECT肿瘤显像剂,值得进一步研究。To develop novel technetium^90Tc^m-labeled thymidine analog for tumor SPECT imaging, two ^90Tc^m-labeled thymidine analogs （99Tcm-ANMdU and 99Tcm-NHT） were synthesized. ^90Tc^m-ANMdU and ^90Tc^m-NHT are stable in aqueous solution and radiochemical purity are over 95%. Biodistribution of^90Tc^m-ANMdU in tumor-bearing mice shows that the high uptake of^90Tc^m-ANMdU in kidney and the clearance is fast. At 60 min p. i. , the ratios of tumor-to-muscle, tumor-to-bone and tumor-to-blood are 1.58 ＋ 0. 17, 1.95 4- 0.31 and 1.17＋0.08, respectively. Biodistribution of ^90Tc^m--NHT in mice shows that the high uptake of 99Tcm-NHT in liver and kidney, indicating that the clearance of ^90Tc^m-NHT is mainly through the hepatobiliary pathway and the renal pathway. At 2 h p. i. , the ratios tumor- to-muscle, tumor-to-bone and tumor-to-blood are 4.41±0. 32, 2.45-0.24 and 1.51±0.18, respectively. These indicate that ^90Tc^m-NHT agent and further study is needed. is probably a potential SPECT tumor imaging agent and further study is needed.

关 键 词：^90Tc^m标记 胸苷衍生物 生物分布 

分 类 号：R817[医药卫生—影像医学与核医学]