^(99)Tc^m-DTPA-双(3,5-二甲氧基-4′-氨基二苯乙烯)的制备及其在小鼠体内的生物分布  

Preparation and Biodistribution of ^(99)Tc^m-DTPA-di(3,5-dimethoxy-4′-aminostilbene)

作　　者：周莲[1] 罗世能[2] 郭雪花[1] 谢敏浩[2] 王洪勇[2] 刘娅灵[2] 邹霈[2] 何拥军[2] 

机构地区：[1]江南大学化学与材料工程学院,江苏无锡214036 [2]江苏省原子医学研究所,江苏无锡214063

出　　处：《同位素》2007年第2期68-72,共5页Journal of Isotopes

基　　金：吴阶平医学基金会资助项目(320675006115)

摘　　要：通过3,5-二甲氧基-4′-氨基二苯乙烯与DTPA双酸酐(DTPAA)反应制备了DTPA-双(3,5-二甲氧基-4′-氨基二苯乙烯),所得产品经IR、MS1、HNMR和元素分析进行结构确认;对其进行了99Tcm标记并观察了标记物在小鼠体内的分布。结果显示,标记物标记率和放化纯度均>90%,在连续观察的6 h内,其放化纯度均>90%,表明其稳定性良好。标记物在小鼠体内的生物分布结果显示,标记物在肝中摄取较高,注射后10 min时达到峰值13.12%/g,且滞留时间较长,注射后180 min时仍有12.07%/g;在肺和血液中清除较快,注射后5 min时分别为10.41%/g和13.50%/g,注射后180 min时则分别降至2.42和2.71%/g。这为进一步研究既能抑制癌细胞,又能对其疗效进行检测的新型放射性治疗药物提供了思路。DTPA-di （3,5-dimethoxy-4＇-aminostilbene） is synthesized by the incorporation of 3,5-dimethoxy-4＇-aminostilbene into DTPAA, and its structure is confirmed by IR, MS, HNMR and element analysis. It is labeled with ^99Tc^m and the biodistribution in rats is also studied. The results show that its labeling yield and radiochemical purity are over 90% repectively and the labeled compound has good stability in vitro after 6 h in room temperature. The results of biodistribution in rats show that the liver uptake of the labeling compound is up to a peek of 13.12%/g at 10 min after injection and the uptake is still 12.07%/ g at 180 min after injection. However it had quick elearance in lung and blood. The uptake values of lung and blood are 10.41 and 13.50%/g at 5 min after injection, respectively and they decreased to 2.42%/g and 2.71%/g at 180 rain after injection, respectively. All of the above mentioned results offere benefial datas for further study on the anti-cancer medicaments and new radiopharmaceuticals.

关 键 词：^99Tc^m- DTPA-双(3 5-二甲氧基-4’-氨基二苯乙烯) 生物分布 

分 类 号：TQ463.7[化学工程—制药化工] R817[医药卫生—影像医学与核医学]