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丁酮肟及酰胺磷定对大鼠血液中梭曼消除的影响
引用本文:应翔宇,阮金秀.丁酮肟及酰胺磷定对大鼠血液中梭曼消除的影响[J].中国药理学与毒理学杂志,2001,15(1):65-67.
作者姓名:应翔宇  阮金秀
作者单位:北京毒物药物研究所, 北京 100850
摘    要:采用电鳐胆碱酯酶抑制法测定大鼠血液中梭曼残留浓度 ,考察了丁酮肟 (DAM)及酰胺磷定 (HI 6)对大鼠血液中梭曼消除的影响 .结果表明 ,4 15μg·kg- 1梭曼 ( 5LD50 )iv后 3min ,DAM预处理有加速梭曼在大鼠血液中消除的趋势 ,使血中梭曼浓度由( 86± 2 2 ) μg·L- 1下降到 ( 53± 9) μg·L- 1,这可能与DAM加速了大鼠体内主要解毒器官中膦酰化羧酸酯酶 (CaE)的脱膦酰化速率有关 ,使有限的酶分子结合了更多的梭曼 .相比之下 ,HI 6预处理则对大鼠血液中梭曼浓度没有明显影响 .提示在大鼠体内 ,CaE对梭曼的解毒作用比胆碱酯酶更为重要

关 键 词:梭曼  羧酸酯酶  胆碱酯酶  重活化剂  丁酮肟  酰胺磷定  代谢解毒  药物
收稿时间:2000-4-26

Effects of diacetylmonoxime and HI-6 on soman clearance from blood in rats
YING Xiang-Yu, RUAN Jin-Xiu.Effects of diacetylmonoxime and HI-6 on soman clearance from blood in rats[J].Chinese Journal of Pharmacology and Toxicology,2001,15(1):65-67.
Authors:YING Xiang-Yu  RUAN Jin-Xiu
Institution:(Beijing Institute of Pharmacology and Toxicology, Beijing 100850, China)
Abstract:The effects of both carboxylesterase reactivator,diacetylmonoxime(DAM) and cholinesterase reactivator, HI-6 on the disappearance of soman from blood in rats intoxicated with soman(415 μg.kg-1,5 LD50,iv) were studied using electric-eel acetylcholinesterase-based microassay. In rats pretreated with DAM the soman concentration was significantly reduced during 3-10 min, which might be partly due to its reactivation of carboxylesterase in detoxifying organs, and thereby increased efficacy of endogenous detoxifying enzymes. By contrast, HI-6 had negligible effects on soman clearance from blood in rats. It suggests that carboxylesterase is more important than cholinesterase in soman detoxification in rats.
Keywords:soman  carboxylesterase  cholinesterase  reactivator  diacetylmonoxime  pyramidoxime  metabolic detoxication  drug
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