螯合剂对小鼠钴（II）急性毒性的解毒效果比较。

Comparison of antidotal efficacy of chelating agents upon acute toxicity of Co(II) in mice.

作者信息

Llobet J M, Domingo J L, Corbella J

出版信息

Res Commun Chem Pathol Pharmacol. 1985 Nov;50(2):305-8.

Abstract

The relative efficacy of 14 chelating agents in alleviating acute cobalt (II) chloride (ip) intoxication has been determined. For a level of 0.70 mmol/kg ip of CoCl2 (slightly higher than its LD50), the ip administration of chelating agents at a 2:1 and 5:1 mole ratio resulted in a significant antidotal action for L-cysteine, N-acetyl-cysteine, L-histidine,glutathione,D,L-penicillamine, DMSA, DTPA and EDTA. For a level of 1.18 mmol/kg ip of CoCl2 (slightly higher than its LD99) only L-cysteine, N-acetylcysteine,glutathione, DMSA, DTPA and EDTA resulted in a significant enhancement of the survival rate. The therapeutic indices of these compounds were respectively: 8.3, 11.8, 10.9, 9.1, 20.5 and 26.4; with EDTA and DTPA being the most effective. However, due to their low toxicity, N-acetylcysteine and glutathione should be considered as possible alternatives.

摘要

已测定了14种螯合剂在缓解急性氯化钴（腹腔注射）中毒方面的相对疗效。对于腹腔注射0.70 mmol/kg的CoCl₂水平（略高于其半数致死量），以2:1和5:1的摩尔比腹腔注射螯合剂时，L-半胱氨酸、N-乙酰半胱氨酸、L-组氨酸、谷胱甘肽、D,L-青霉胺、二巯基丁二酸（DMSA）、二乙三胺五乙酸（DTPA）和乙二胺四乙酸（EDTA）产生了显著的解毒作用。对于腹腔注射1.18 mmol/kg的CoCl₂水平（略高于其99%致死量），只有L-半胱氨酸、N-乙酰半胱氨酸、谷胱甘肽、DMSA、DTPA和EDTA显著提高了存活率。这些化合物的治疗指数分别为：8.3、11.8、10.9、9.1、20.5和26.4；其中EDTA和DTPA最为有效。然而，由于N-乙酰半胱氨酸和谷胱甘肽毒性较低，应考虑将它们作为可能的替代药物。