甲氟膦酸环己酯与甲氟膦酸异丙酯合用在试管内对大鼠脑乙酰胆碱酯酶的抑制及其重活化

为进一步了解甲氟膦酸环己酯(GF)与甲氟膦酸异丙酯(GB)的联合特性,为制订医学防护措施提供更多的理论依据, 用微量DTNB法对GF，GB和GF与GB混合对大鼠脑乙酰胆碱酯酶(AChE)的抑制及肟类重活化剂酰胺磷定（HI-6）和氯磷定（2-PAM-Cl）的重活化作用进行了研究. 结果表明, GF，GB和GF与GB混合抑制90%左右AChE活力的终浓度分别为 3.98, 39.8和21.9 nmol·L^-1, pI₅₀ 分别为10.3， 9.1和9.2. GF与GB合用对AChE的抑制强度未见增加. HI-6对AChE的抑制有较强的重活化作用,与2-PAM-Cl比较有显著差异. HI-6和2-PAM-Cl对GF与GB合用的重活化比单独的GF更容易.

Inhibition and reactivation of rat brain acetylcholinesterase activity by combined cyclohexyl- and isopropyl-methylphosphonofluoridate in vitro

In order to further understand combining characteristic of cyclohexyl methylphosphonofluoridate(GF) and isopropyl methylphosphonofluoridate (GB) and contribute more scientific data for its medical protection, the potency of inhibition of acetylcholinesterase (AChE) activity induced by GF, GF+GB and the effects of reactivation by oximes pyramidoxime monohydrate(HI-6) and pyridine-2-aldoxime methylchloride(2-PAM-Cl) in rat brain were investigated with DTNB microanalysis in this study. The results showed that GF(3.98 nmol·L^-1), GB(39.8 nmol·L^-1) and GF+GB (21.9 nmol·L^-1) inhibit AChE activity by about 90 percent. The values of their pI₅₀ are 10.3, 9.1 and 9.2, respectively. The combination of two nerve agents did not result in potentiation of AChE inhibition. Both HI-6 and 2-PAM-Cl could efficiently reactivate GF or GF+GB, although the reactivation rate of HI- 6 was higher than that of 2-PAM-Cl.