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小鼠一次灌胃二巯基丁二酸(DMSA)混悬剂的LD_(50)为6g/kg,大白鼠为4g/kg。正常狗每天灌DMSA0.5g/kg共6周(5天/周)给药后食量减少,呕吐,体重减轻。血象、血糖、心电图、肝功能和肾功能均无显著变化。解剖一狗见十二脂肠有少量充血。灌服0.2g/kg组无明显症状。兔一次灌服DMSA后半小时,血中SH含量达高峰,5小时内血中SH浓度已明显下降。 小鼠皮下注射~(210)Pb-醋酸铅后以骨和肾~(210)Pb含量最高。静注二巯基丁二酸钠(Na-DMS)或灌服DMSA可排除体内吸收~(210)Pb,二者均非常显著降低骨和肾中~(210)Pb。 兔皮下注射硫酸铜后,DMSA可明显促进尿铜的排泄。加服NaHCO_3或枸橼酸钠可加强DMSA的排铜作用。 小鼠分别肌注~(125)Sb-吐酒石、~(90)Sr-硝酸锶、~(204)Tl-硫酸亚铊和~(147)Pm-硝酸钷后立即灌胃DMSA和NaHCO_3,DMSA明显增加放射性金属在尿中排泄。促使~(125)Sb排泄增加6倍、~(90)Sr 2倍、~(204)Tl 11倍和可提高~(147)Pm 12倍。血和大多组织中放射性都有降低。 上述结果提示口服DMSA可用于金属中毒治疗。DMSA比Na-DMS稳定低毒,值得继续研究。
The mice were once intragastric dithiol succinic acid (DMSA) suspension LD_ (50) 6g / kg, rats 4g / kg. Normal dogs daily irrigation DMSA0.5g / kg for 6 weeks (5 days / week) after administration reduced appetite, vomiting, weight loss. Blood, blood glucose, ECG, liver function and renal function were not significantly changed. Anatomy of a dog saw a small amount of 12 intestine congestion. No obvious symptoms were found in the group fed 0.2g / kg. After a half-hour administration of DMSA in rabbits, the SH content in the blood peaked and the SH concentration in the blood dropped significantly within 5 hours. The highest content of ~ (210) Pb in bone and kidney was found after subcutaneous injection of ~ (210) Pb-lead acetate in mice. Intravenous sodium dimercaptosuccinate (Na-DMS) or DMSA was administered to excrete ~ (210) Pb in vivo, both of which significantly reduced ~ (210) Pb in bone and kidney. Subcutaneous injection of copper sulfate in rabbits, DMSA can significantly promote urinary copper excretion. Adding NaHCO_3 or sodium citrate can enhance the copper discharge of DMSA. DMSA and NaHCO 3 were intragastrically administered intramuscularly to ~ (125) Sb-tartar, ~ (90) Sr-strontium nitrate, ~ (204) Tl-thallous sulphate and ~ (147) Pm- DMSA significantly increases the excretion of radioactive metals in the urine. It promoted the excretion of ~ (125) Sb by 6 times, ~ (90) Sr 2 times, ~ (204) Tl 11 times and ~ 147 147 Pm 12 times. Radioactivity in blood and most tissues is reduced. These results suggest that oral DMSA can be used for metal poisoning treatment. DMSA is more stable and less toxic than Na-DMS and deserves further study.