Saji H, Yokoyama A, Hata N, Misaki A, Tanaka H, Morita R, Fukunaga M, Torizuka K
Radioisotopes. 1980 Jan;29(1):7-12. doi: 10.3769/radioisotopes.29.7.
Chelating agent, such as CaEDTA, CaDTPA, D-penicillamine, DMSA, desferoxamine, NTA, cysteine ethyl ester, BAL, alpha-MPG, phthalein complexone, were tested as a possible contrast enhancing agent for tumor imaging with 67Ga-citrate. The intravenous administration of a chelating agent to Ehrlich's tumor bearing mice, one hour after the injection of 67Ga-citrate, accelerated the blood clearance with only a very slight change of activity in the target, increasing the tumor-to-blood ratio, and consequently achieving a better visualization. Among the tested chelating agents, D-penicillamine showed the highest target-to-nontarget ratio at a shorter time: a good tumor-to-blood ratio, performed after 24 hr with non-treated animals, was achieved in only 1-3 hr with post-treated animals. Thus, D-penicillamine hold a considerable promise as a contrast enhancing agent for future clinical use.
螯合剂,如CaEDTA、CaDTPA、D-青霉胺、二巯基丁二酸(DMSA)、去铁胺、氮川三乙酸(NTA)、半胱氨酸乙酯、二巯丙醇(BAL)、α-甲氧基苯妥英、酞菁络合酮,作为一种可能的造影剂用于67Ga-柠檬酸盐肿瘤显像进行了测试。在注射67Ga-柠檬酸盐1小时后,对荷艾氏瘤小鼠静脉注射螯合剂,加快了血液清除速度,靶区活性仅有非常轻微的变化,提高了肿瘤与血液的比值,从而实现了更好的显像。在所测试的螯合剂中,D-青霉胺在较短时间内显示出最高的靶与非靶比值:未处理动物在24小时后获得的良好肿瘤与血液比值,在处理后的动物中仅1 - 3小时就实现了。因此,D-青霉胺作为一种造影剂在未来临床应用中有很大的前景。