Bajgar J, Fusek J, Patocka J, Hrdina V
Acta Biol Med Ger. 1977;36(2):231-6.
A modification for continual monitoring of the blood acetylcholinesterase activity in the rat on an auto analyzer system was described. With using this technique, inhibition of the enzyme in vitro with O-ethyl-S-(2-dimethylaminoethyl)-methylphosphonothioate was determined. Bimolecular rate constant and I50 values were 1.66-10(6) M-1-min-1 and 1.4-10(-8)M, respectively. Rats treated i.m. with 0.043 mg/kg of this compound showed fast and rapid inhibition of the blood acetylcholinesterase after intoxication. The bimolecular rate constant of inhibition in vivo, calculated analogously as that in vitro was 1.37-10(6) M-1-min-1. On the presumption that both rates of inhibition (in vitro and in vivo) are identical, the concentration of organophosphate producing inhibition effect in vivo was 82% of the dose administered.
描述了一种在自动分析仪系统上连续监测大鼠血液乙酰胆碱酯酶活性的改进方法。使用该技术，测定了O-乙基-S-(2-二甲基氨基乙基)-甲基硫代磷酸酯对体外酶的抑制作用。双分子速率常数和I50值分别为1.66×10⁶ M⁻¹·min⁻¹和1.4×10⁻⁸ M。经肌肉注射0.043 mg/kg该化合物处理的大鼠在中毒后血液乙酰胆碱酯酶表现出快速抑制。体内抑制的双分子速率常数，按照与体外类似的方法计算为1.37×10⁶ M⁻¹·min⁻¹。假定体外和体内的抑制速率相同，体内产生抑制作用的有机磷酸酯浓度为给药剂量的82%。
