高等学校化学学报

高等学校化学学报

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两种新型99mTcN核标记的甲硝唑类乏氧显像剂的制备及生物性能评价

陆洁, 孔德靖, 许明炎, 王学斌   

  1. 放射性药物教育部重点实验室, 北京师范大学化学学院, 北京 100875
  • 收稿日期:2008-06-24 修回日期:1900-01-01 出版日期:2009-02-10 发布日期:2009-02-10
  • 通讯作者: 陆洁

Preparation and Biological Evaluation of Two Novel 99mTc-nitrido Complexes of Metronidazole Derivative for Targeting Hypoxia

LU Jie*, KONG De-Jing, XU Ming-Yan, WANG Xue-Bin

  

  1. Key Laboratory of Radiopharmaceuticals, Ministry of Education, College of Chemistry, Beijing Normal University, Beijing 100875, China
  • Received:2008-06-24 Revised:1900-01-01 Online:2009-02-10 Published:2009-02-10
  • Contact: LU Jie

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摘要： 为研制新的肿瘤乏氧显像剂, 设计合成了2-(2-甲基-5-硝基咪唑基)乙基氨荒酸钾(MNIE-DTC)和4-(2-甲基-5-硝基咪唑基)丁基氨荒酸钾(MNIB-DTC)两种氨荒酸盐配体, 并制得了相应的99mTcN核配合物99mTcN(MNIE-DTC)2和99mTcN(MNIB-DTC)2. 所获得的两种99mTcN核配合物均为电中性, 具有较高的体外稳定性. 在荷乳腺癌的TA-2小鼠体内分布实验结果显示, 两种配合物均具有一定的肿瘤摄取, 给药1 h后, 99mTcN(MNIE-DTC)2和99mTcN(MNIB-DTC)2的肿瘤摄取率分别为(0.50±0.01)%ID/g和(0.64±0.10)%ID/g. 注入肼苯哒嗪后, 两种配合物的肿瘤摄取明显增高, 表明这两种配合物都具有对乏氧肿瘤的选择性.

关键词: 99mTcN核配合物, 肿瘤乏氧显像剂, 甲硝唑

Abstract: In order to develop new tumor hypoxia imaging agent, two novel dithiocarbamate ligands, potassium 2-(2-methyl-5-nitro-1H-imidazolyl)-ethyl-carbamate(MNIE-DTC) and potassium 4-(2-methyl-5-nitro-1H-imidazolyl)-butyl-carbamate(MNIB-DTC), and the corresponding 99mTcN-complexes were prepared. Both neutral complexes were stable in vitro. Biological evaluation in TA-2 mice bearing MA891 tumor showed that both [99mTcN(MNIE-DTC)2] and [99mTcN(MNIB-DTC)2] had certain tumor uptakes of (0.50±0.01)%ID/g and (0.64±0.10)%ID/g at 1 h post-injection, respectively. A significant increase in tumor uptakes of both complexes were produced by injection of hydralazine. The results indicated that the two complexes could be selectively accumulated in hypoxic tumors.

Key words: 99mTc-nitrodo complexes, Tumor hypoxia imaging agent, Metronidazole

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