中文摘要：

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）：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1h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．

英文摘要：

In order to develop new tumor hypoxia imaging agent, two novel dithiocarbamate ligands, potassi- um 2- （ 2-methyl-5-nitro-1 H-imidazolyl） -ethyl-earbamate （ MNIE-DTC ） and potassium 4- （ 2-methyl-5-nitro-1 H- imidazolyl）-butyl-carbamate （MNIB-DTC）, and the corresponding ^99mTcN-eomplexes were prepared. Both neutral complexes were stable in vitro. Biological evaluation in TA-2 mice bearing MA891 tumor showed that both [ ^99mTeN （MNIE-DTC） 2 3 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.