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拮抗剂对大鼠有机磷酸酯急性毒性影响的定量研究。

Quantitative studies of the effect of antagonists on the acute toxicity of organophosphates in rats.

作者信息

Natoff I L, Reiff B

出版信息

Br J Pharmacol. 1970 Sep;40(1):124-34. doi: 10.1111/j.1476-5381.1970.tb10617.x.

Abstract
  1. The subcutaneous acute toxicities of the vinyl phosphate pesticides monocrotophos, dicrotophos, chlorfenvinphos, crotoxyphos, dichlorvos, mevinphos, and of the experimental compounds SD 4455 (cis-2-carboxy-1-methylvinyl dimethylphosphate) and SD 7779 (cis-2-(1-phenylethoxy) carbonyl-1-methylvinyl diethylphosphate) have been determined in female rats.2. The effects on the log dose-probit mortality curves to the vinylphosphates of the therapeutic subcutaneous administration of methylatropine, atropine, N-methylpyridinium-2-aldoxime methanesulphonate and obidoxime have been studied.3. Elevation of the LD50 values by the therapeutic regimens was shown to be an unsatisfactory measure of therapeutic efficiency, while reduction of the effect of a maximally lethal dose (LD90) to less than that of a minimally lethal dose (LD10) provided a better quantitative measure of therapeutic efficiency.4. The combination of atropine sulphate (50 mumol base/kg) with obidoxime (250 mumol/kg) was found to be generally the most effective of the antidotal regimens.
摘要
  1. 已在雌性大鼠中测定了磷酸乙烯酯农药久效磷、百治磷、毒虫畏、巴毒磷、敌敌畏、速灭磷,以及实验化合物SD 4455(顺式-2-羧基-1-甲基乙烯基二甲基磷酸酯)和SD 7779(顺式-2-(1-苯乙氧基)羰基-1-甲基乙烯基二乙基磷酸酯)的皮下急性毒性。

  2. 研究了皮下注射治疗剂量的甲基阿托品、阿托品、氯解磷定和双复磷对磷酸乙烯酯的对数剂量-概率死亡率曲线的影响。

  3. 治疗方案使半数致死剂量(LD50)值升高,这被证明是衡量治疗效果的一个不令人满意的指标,而将最大致死剂量(LD90)的效应降低到小于最小致死剂量(LD10)的效应,则提供了一个更好的衡量治疗效果的定量指标。

  4. 发现硫酸阿托品(50 μmol碱/kg)与双复磷(250 μmol/kg)联合使用通常是最有效的解毒方案。

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Parathion metabolism in female rat.雌性大鼠体内对硫磷的代谢
Arch Int Pharmacodyn Ther. 1959 Feb 1;118(3-4):308-16.
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Chemical reactivation of phosphorylated human and bovine true cholinesterases.磷酸化人及牛真性胆碱酯酶的化学再活化
Br J Pharmacol Chemother. 1956 Sep;11(3):295-303. doi: 10.1111/j.1476-5381.1956.tb01069.x.

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