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首页> 外文期刊>Journal of enzyme inhibition and medicinal chemistry. >In vitro reactivation of sarin-inhibited brain acetylcholinesterase from different species by various oximes.
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In vitro reactivation of sarin-inhibited brain acetylcholinesterase from different species by various oximes.

机译:通过各种肟对不同物种的沙林蛋白抑制的脑乙酰胆碱酯酶进行体外再活化。

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摘要

In vitro as well as in vivo evaluation of the reactivating efficacy of various oximes against nerve agent-inhibited acetylcholinesterase has been usually done with the help of animal experiments. Nevertheless, previously published data indicate that the reactivation potency of oximes may be different in human and animal species, which may hamper the extrapolation of animal data to human data. Therefore, to better evaluate the efficacy of various oximes (pralidoxime, obidoxime, HI-6, K033) to reactivate brain acetylcholinesterase inhibited by sarin by in vitro methods, human, rat and pig brain acetylcholinesterase were used to calculate kinetic parameters for the reactivation. Our results show differences among the species, depending on the type of oxime, and indicate that data from animal experiments needs to be carefully evaluated before extrapolation to humans.
机译:通常在动物实验的帮助下,进行了各种肟对神经药抑制的乙酰胆碱酯酶的活化效果的体外和体内评价。然而,先前发表的数据表明,肟在人类和动物物种中的重新激活能力可能有所不同,这可能会阻碍动物数据向人类数据的外推。因此,为了通过体外方法更好地评估各种肟(普利多肟,奥比多肟,HI-6,K033)重新激活沙林蛋白抑制的脑乙酰胆碱酯酶的功效,使用人,大鼠和猪的脑乙酰胆碱酯酶来计算该激活的动力学参数。我们的结果显示了不同物种之间的差异,具体取决于肟的类型,并表明动物实验数据需要外推到人类之前需要仔细评估。

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