Prozorovskiĭ V B, Khramova E A, Ardab'eva T V
Biull Eksp Biol Med. 1983 Oct;96(10):66-8.
HI-6 and TMB-4 were the most effective and safe of 7 cholinesterase reactivators tested as agents for the prophylaxis of proserine poisoning of male mice. The reactivator HI-6 strongly potentiated the prophylactic efficacy of a mixture of atropine and arpenal administered in the doses sufficient for the blockade of both the m- and h-cholinoreactive systems of mice. As demonstrated by experiments in vitro, HI-6 and TMB-4 did not reacivate proserine-inhibited cholinesterase. The natural anticholinesterase activity of HI-6 was negligible. Based on the correlation of the data obtained to the reported data indicating that HI-6 has a low ganglioblocking activity it is inferred that the direct effect on the receptor is of no importance for the potentiating effect. It is assumed that HI-6 modulates the cholinoreactive systems, which leads to a dramatic increase of the efficacy of cholinolytics.
在作为雄性小鼠预防毒扁豆碱中毒药物进行测试的7种胆碱酯酶复活剂中，HI-6和TMB-4是最有效且最安全的。复活剂HI-6能显著增强以足以阻断小鼠M和H胆碱反应系统的剂量给药的阿托品和阿品那混合物的预防效果。体外实验表明，HI-6和TMB-4不能使被毒扁豆碱抑制的胆碱酯酶重新活化。HI-6的天然抗胆碱酯酶活性可忽略不计。根据所得数据与报告数据的相关性，报告数据表明HI-6具有低神经节阻断活性，由此推断对受体的直接作用对增强作用并不重要。据推测，HI-6可调节胆碱反应系统，从而导致抗胆碱药的疗效显著提高。
