^(99)Tc^m-BnAO-乙二醇独甲醚的合成及其生物分布  

Synthesis,Radiolabeling and Biodistribution of ^(99)Tc^m-BnAO Ethylene Glycol Monoethyl Ether Derivate

作　　者：黄华璠 周浩[1] 黄士堂[1] 褚泰伟[1] 

机构地区：[1]北京大学化学与分子工程学院放射化学与辐射化学重点学科实验室北京分子科学国家实验室,北京100871

出　　处：《同位素》2011年第1期29-33,共5页Journal of Isotopes

基　　金：国家自然科学基金资助项目(20771011;21071010)

摘　　要：99Tcm-BnAO(HL91)是一种非硝基咪唑类乏氧显像剂,为了提高其乏氧显像性能,合成了BnAO-乙二醇独甲醚,并对其进行了99Tcm标记。结果表明,99Tcm-BnAO及99Tcm-BnAO-乙二醇独甲醚均为电中性,99Tcm-BnAO-乙二醇独甲醚脂溶性有所提高。其荷S180瘤小鼠体内生物分布结果表明,随着时间的延长,99Tcm-BnAO及99Tcm-BnAO-乙二醇独甲醚在肿瘤组织的相对摄取率逐渐增加。但99Tcm-BnAO-乙二醇独甲醚的肿瘤与血和肿瘤与肌肉的放射性摄取比(T/NT)较99Tcm-BnAO略有降低。Hypoxic cells within a tumor is associated with the radiotherapy and chemotherapy resistance.The development of noninvasive methods for detecting hypoxia is need.99Tcm-BnAO is a non-nitroimidazole imaging agent for hypoxia,and has been evaluated both in vitro and in vivo as a noninvasive marker.In order to improve its ability for imaging,the ligand BnAO was modified with ethylene glycol monoethyl ether（EGME） on both sides.BnAO and BnAO-EGME were labeled with 99Tcm.99Tcm-BnAO and 99Tcm-BnAO-EGME were found to be electrically neutral at physiological condition by paper electrophoresis.99Tcm-BnAO-EGME showed higher hydrophilicity in octanol/water partition coefficient experiment and better stability in vitro.The biodistribution in mice bearing S180 tumor demonstrated that 99Tcm-BnAO and 99Tcm-BnAO-EGME could accumulate in tumor with time going.However,it was found that 99Tcm-BnAO-EGME showed a little disadvantage in the ratio tumor to blood and the ratio of tumor to muscle compared with 99Tcm-BnAO.

关 键 词：99Tcm-BnAO 乙二醇独甲醚 生物分布 

分 类 号：TQ463.7[化学工程—制药化工] R817.9[医药卫生—影像医学与核医学]