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99Tcm-BnAO-乙二醇独甲醚的合成及其生物分布

黄华璠 周浩 黄士堂 褚泰伟

同位素2011,Vol.24Issue(1):29-33,5.
同位素2011,Vol.24Issue(1):29-33,5.

99Tcm-BnAO-乙二醇独甲醚的合成及其生物分布

Synthesis, Radiolabeling and Biodistribution of 99Tcm-BnAO Ethylene Glycol Monoethyl Ether Derivate

黄华璠 1周浩 1黄士堂 1褚泰伟1

作者信息

  • 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
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摘要

Abstract

Hypoxic cells within a tumor is associated with the radiotherapy and chemotherapy resistance. The development of noninvasive methods for detecting hypoxia is need.99 Tcm-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 BnAOwas 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

Key words

99Tcrm-BnAO/ ethylene glycol monoethyl ether/ biodistribution

分类

能源科技

引用本文复制引用

黄华璠 ,周浩,黄士堂,褚泰伟..99Tcm-BnAO-乙二醇独甲醚的合成及其生物分布[J].同位素,2011,24(1):29-33,5.

基金项目

国家自然科学基金资助项目(20771011,21071010) (20771011,21071010)

同位素

OACSTPCD

1000-7512

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