Protas L L, Muske G A, Mndzhoian O L, Danilov A F, Mikhel'son M Ia
Farmakol Toksikol. 1975 May-Jun;38(3):298-303.
Inhibition of active cholinesterases in cats with armine or the GT-165 compound (0,0-diethyl-S-/beta-arylmethylamino) ethyl/thiophosphate methylsulphomethylate) potentiases ten- and hundred-fold the blocking action of subecholine and its derivatives on the neuro-muscular condution. The cholinesterase reactivator dipyroxime (2-5 mg/kg) quickly lifts the conduction block, provoked by muscle relaxants of the subecholine type under the cholinesterase inhibition. The subecholine analogue with a single propyl radical at each atom of nitrogen does not display any pressor action and, upon inhibition of cholinesterases, it blocks the neuro-muscular conduction when used in a dose of 0.1-0.2 gamma/kg. The maximal potentiation of the blocking action exerted by subecholine and its analogues is achieved in inhibiting not only pseudocholinesterase but acetylcholinesterase as well.
用毒扁豆碱或GT - 165化合物(0,0 - 二乙基 - S - /β - 芳基甲基氨基)乙基/硫代磷酸甲酯)抑制猫体内的活性胆碱酯酶,可使丁酰胆碱及其衍生物对神经 - 肌肉传导的阻断作用增强10倍和100倍。胆碱酯酶复活剂双吡啶肟(2 - 5毫克/千克)能迅速解除在胆碱酯酶抑制情况下丁酰胆碱类肌肉松弛剂所引发的传导阻滞。在每个氮原子上仅带有一个丙基的丁酰胆碱类似物不表现出任何升压作用,并且在胆碱酯酶被抑制时,以0.1 - 0.2微克/千克的剂量使用时会阻断神经 - 肌肉传导。丁酰胆碱及其类似物所产生的阻断作用的最大增强效果是在不仅抑制假性胆碱酯酶而且也抑制乙酰胆碱酯酶时实现的。