羰基锝硝基咪唑化合物^99Tc^m(CO)3-MNLS的标记和生物学评价  

Preparation and Evaluation of a Novel Hypoxic Imaging Agent ^(99)Tc^m(CO)_3-MNLS

作　　者：甘红梅[1] 刘晶莹[1] 査智豪 乔晋萍[1] 朱霖[1] 

机构地区：[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

出　　处：《核化学与放射化学》2011年第5期302-307,共6页Journal of Nuclear and Radiochemistry

基　　金：国家重点基础研究发展规划项目(973计划)(No.2006CB500705);国家高技术研究发展计划资助项目(863计划)(No.2006AA02A408)

摘　　要：本文采用直接标记法在水相中将羰基锝中间体[99 Tcm(CO)3(H2O)3]+与含磷酸基团的硝基咪唑衍生物2-(2-甲基-5-硝基咪唑-1-基)乙基磷酸盐(2-(2-methyl-5-nitro-1H-imidazol-1-yl)ethyl dihydrogen phos-phate,MNLS)配位得到99 Tcm(CO)3-MNLS配合物;研究了99 Tcm(CO)3-MNLS的最佳标记条件、理化性质及其在荷EMT-6肿瘤小鼠体内的生物分布。结果表明,当MNLS质量为10mg、pH=4.0～8.0、80℃下反应15min时,99 Tcm(CO)3-MNLS配合物放化纯度大于99%。电泳试验结果提示,99 Tcm(CO)3-MNLS为水溶性的电中性配合物,具有良好的体外稳定性。动物分布试验显示,99 Tcm(CO)3-MNLS在荷EMT-6肿瘤小鼠体内有较高的肿瘤摄取值,且滞留较好;此外,99 Tcm(CO)3-MNLS较99 Tcm-MNLS在骨中的摄取值明显降低。以上结果为研发新型乏氧组织显像剂提供了重要参考。The labeling method for ^99Tc^m（CO）_3-MNLS was established, and the biodistribu- tion of ^99Tc^m（CO）_3-MNLS in EMT-6 tumor-bearing mice was carried out as well. The optimal labeling condition was found as follows： MNLS 10 mg, pH=4.0-8.0 at 80 ℃ for 15 rain; and the radiochemical purity was more than 99% proved by HPLC. The new radiola-beled compound＇ s stability was good in vitro, and it was electrically neutral and watersoluble. The biodistribution in EMT-6 tumor-bearing mice show that ^99Tc^m（CO）_3-MNLS has a considerable uptake and eligible retention time in tumor, and the bone uptake of ^99Tc^m（CO）_3-MNLS is much lower than ^99Tc^m-MNLS.

关 键 词：[^99Tc^m(CO)_3(H_2O)_3]^+ MNLS ^99Tc^m(CO)_3-MNLS 理化性质 生物分布 

分 类 号：R817[医药卫生—影像医学与核医学]