Cetković S, Cvetković M, Jandrić D, Cosić M, Bosković B
Fundam Appl Toxicol. 1984 Apr;4(2 Pt 2):S116-23. doi: 10.1093/toxsci/4.2part2.116.
It has been shown that HI-6 was the most potent oxime so far known in poisoning by sarin, VX , and soman, but its protective effect in tabun poisoning, allegedly due to poor reactivation of inhibited ChE, was much less pronounced. We have found that the thiocholine-like analog of tabun , O-ethyl, N-N- dimethyamino -S-(2-diethylaminoethyl)- thiophosphatemethylsul fomethylate (Ta-S-N+), was very useful in resolving this problem and established the relationship between reactivating and protective effects of PAM-2 Cl, HI-6, and HGG-12 in rats. PAM-2 Cl (protective ratio (PR) = 22.1) and HI-6 (PR = 24.8), combined with atropine, were very effective against Ta-S-N+ poisoning and reactivating inhibited RBC AChE in vitro and rat blood ChE in vivo. The inefficiency of PAM-2 Cl (PR = 1.6) and HI-6 (PR = 2) in tabun poisoning was due to their inadequacy to reactive tabun -inhibited ChEs . The protective effects of HGG-12 in tabun (PR = 2.8) and Ta-S-N+ poisoning (PR = 2.6) were low, and in the absence of any reactivation of inhibited ChEs , have been attributed to its direct pharmacological effects, which were much more potent in the comparison with PAM-2 Cl or HI-6. It is concluded that the reactivation of inhibited ChE is of decisive importance in the efficient protection in poisoning by tabun and other known chemical warfare nerve agents, whereas their direct pharmacological effects are of limited value, allowing survival of animals only against a few LD50s .
业已表明,HI-6是迄今已知对沙林、VX和梭曼中毒最有效的肟类药物,但据称由于其对被抑制胆碱酯酶(ChE)的重活化效果不佳,它在塔崩中毒中的保护作用要弱得多。我们发现,塔崩的硫代胆碱类似物,O-乙基,N,N-二甲基氨基-S-(2-二乙氨基乙基)硫代磷酸甲酯甲基磺酸甲酯(Ta-S-N+),在解决这一问题方面非常有用,并确立了PAM-2 Cl、HI-6和HGG-12在大鼠体内的重活化作用与保护作用之间的关系。PAM-2 Cl(保护率(PR)=22.1)和HI-6(PR = 24.8)与阿托品联用,对Ta-S-N+中毒非常有效,并且在体外能重活化被抑制的红细胞乙酰胆碱酯酶(AChE),在体内能重活化大鼠血液中的ChE。PAM-2 Cl(PR = 1.6)和HI-6(PR = 2)在塔崩中毒中无效是由于它们不足以重活化被塔崩抑制的ChE。HGG-12在塔崩中毒(PR = 2.8)和Ta-S-N+中毒(PR = 2.6)中的保护作用较低,并且在未对被抑制的ChE进行任何重活化的情况下,其保护作用被归因于其直接药理作用,与PAM-2 Cl或HI-6相比,这种直接药理作用要强得多。结论是,对于塔崩和其他已知化学战神经毒剂中毒的有效保护而言,重活化被抑制的ChE具有决定性意义,而它们的直接药理作用价值有限,仅能使动物在少数半数致死剂量(LD50)下存活。