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首页> 外文期刊>Journal of applied toxicology >Effect of some acetylcholinesterase reactivators on human platelet aggregation in vitro.
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Effect of some acetylcholinesterase reactivators on human platelet aggregation in vitro.

机译:某些乙酰胆碱酯酶活化剂对人血小板聚集的影响。

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Acetylcholinesterase (AChE) reactivators are employed for the prophylaxis and treatment of intoxications with organophosphorus AChE inhibitors, including nerve agents and pesticides. For the recovery of inhibited enzyme, derivatives from the group of pyridinium or bispyridinium aldoximes (called oximes) are used. Adverse effects of these substances are not well elucidated, because of their narrow and one-shot usage. Owing to this fact, the study evaluated the influence of some currently applied oximes on human platelet aggregation in vitro. The antiplatelet activity of pralidoxime, obidoxime, HI-6, methoxime and HLo 7 was assayed in human platelet rich plasma (2.5 x 10(8) platelets.ml(-1)) at a concentration of 1.35 mM. Arachidonic acid (AA), adenosine diphosphate (ADP), collagen (COL) and thrombin (TR) were used as agonists of platelet aggregation. All tested substances, except pralidoxime and methoxime, caused a significant inhibition of the aggregation process induced by AA, ADP and COL. Of the oximes assayed, none was found to influence TR triggered aggregation. Since reduced platelet aggregation can play an important role as an adverse effect in reactivator administration, further evaluation is needed for the estimation of the real impact of active oximes to the aggregation process in humans.
机译:乙酰胆碱酯酶(AChE)活化剂用于预防和治疗有机磷AChE抑制剂(包括神经毒剂和杀虫剂)中毒。为了回收抑制的酶,使用了吡啶鎓或双吡啶醛醛肟类的衍生物(称为肟)。由于它们的使用范围很窄而且只能一次性使用,因此尚未很好地阐明这些物质的不良影响。由于这一事实,该研究评估了一些目前使用的肟在体外对人血小板聚集的影响。在人血小板丰富的血浆(2.5 x 10(8)血小板.ml(-1))中以1.35 mM的浓度测定了普利昔肟,奥比多肟,HI-6,甲氧肟和HLo 7的抗血小板活性。花生四烯酸(AA),二磷酸腺苷(ADP),胶原蛋白(COL)和凝血酶(TR)被用作血小板聚集的激动剂。除普利昔肟和甲氧肟外,所有测试物质均显着抑制了由AA,ADP和COL诱导的聚集过程。在所测定的肟中,未发现任何会影响TR引发的聚集。由于减少的血小板聚集可在再活化剂管理中起不利作用而起重要作用,因此需要进一步评估来评估活性肟对人类聚集过程的实际影响。

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