【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.更多还原

【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.更多还原