van Helden H P, van der Wiel H J, Wolthuis O L
Br J Pharmacol. 1983 Mar;78(3):579-89. doi: 10.1111/j.1476-5381.1983.tb08818.x.
1 The ability of various bis-pyridinium oximes to restore organophosphate-inhibited neuromuscular transmission in vitro was compared in human intercostal and marmoset diaphragm muscles. 2 HI-6 (2-hydroxyiminomethyl-pyridinium-1-methyl-4'-carbamoyl-pyridinium-1'-methyl ether dichloride monohydrate) appeared very effective against VX (O-ethyl S-2-diisopropylaminoethyl methylphosphonothioate) and sarin in both muscles, whereas obidoxim was quite effective against tabun. 3 Against soman, HI-6, HS-6 (2-hydroxyiminomethyl-pyridinium-1-methyl-3'-carbamoyl-pyridinium-1'-methyl ether dichloride dihydrate) and obidoxim had little effect in the human muscle and only slight activity in the marmoset muscle; HGG-12 (2-hydroxyiminomethyl-pyridinium-1-methyl-3'-phenylcarbonyl-pyridinium-1'-methy l ether dichloride) and benzyl-P2A (1-benzyl-2-hydroxyiminomethyl-pyridinium methanesulphonate) were ineffective. 4 Anaesthetized, atropinized marmosets were poisoned with soman (4 X LD50, i.v.) and subsequently treated with HI-6, HS-6 or HGG-12. Only HI-6 and HS-6 were marginally effective in restoring respiration and neuromuscular transmission. 5 Marmoset muscle is a reasonable model for human muscle for the study of organophosphate poisoning and therapy.
1 在人肋间肌和狨猴膈肌中比较了各种双吡啶肟在体外恢复有机磷酸酯抑制的神经肌肉传递的能力。2 HI-6(2-羟基亚氨基甲基吡啶-1-甲基-4'-氨基甲酰基吡啶-1'-甲基醚二氯化物一水合物)在两种肌肉中对VX(O-乙基 S-2-二异丙基氨基乙基甲基硫代膦酸酯)和沙林似乎非常有效,而双复磷对塔崩相当有效。3 对于梭曼,HI-6、HS-6(2-羟基亚氨基甲基吡啶-1-甲基-3'-氨基甲酰基吡啶-1'-甲基醚二氯化物二水合物)和双复磷在人肌肉中几乎没有作用,在狨猴肌肉中只有轻微活性;HGG-12(2-羟基亚氨基甲基吡啶-1-甲基-3'-苯基羰基吡啶-1'-甲基醚二氯化物)和苄基-P2A(1-苄基-2-羟基亚氨基甲基吡啶甲磺酸盐)无效。4 对麻醉、用阿托品处理的狨猴静脉注射梭曼(4×LD50)使其中毒,随后用HI-6、HS-6或HGG-12进行治疗。只有HI-6和HS-6在恢复呼吸和神经肌肉传递方面有微弱效果。5 狨猴肌肉是研究有机磷酸酯中毒和治疗的人类肌肉的合理模型。