首页> 外文期刊>European journal of drug metabolism and pharmacokinetics >Influence of different calcic antagonists on the Caco-2 cell monolayer integrity or 'TEER, a measurement of toxicity?'.
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Influence of different calcic antagonists on the Caco-2 cell monolayer integrity or 'TEER, a measurement of toxicity?'.

机译:不同的钙离子拮抗剂对Caco-2细胞单层完整性或“ TEER,毒性的测定?”的影响。

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摘要

The purpose of this work was to investigate the interest of the TEER measurement, a quite simple measure, as an evaluation of toxicity, in function of time and level of drug in the experimental medium, for different anticalcic agents. The extend of the increase and decrease of TEER, was evaluated by measuring the TEERmax and calculating the TEER50 respectively. Three groups of compounds could be therefore considered. The first, characterized by a quite short period of TEER increase, followed by an extremely rapid decrease (high values of TEER50), included perhexiline and prenylamine. The most toxic compounds, the second one, characterized by the smallest variations of TEER, included verapamil and diltiazem. This group was related with the less toxic compounds, the third group, represented by bepridil, characterized by dependant-dose TEERmax and TEER50. Therefore, the TEER measurement appeared as a quite simple approach of comparative toxicity of anticalcic agents.
机译:这项工作的目的是研究针对不同抗钙剂的TEER测量的兴趣,TEER测量是一种非常简单的测量方法,用于评估毒性,时间和实验介质中药物水平的函数。通过分别测量TEERmax和计算TEER50来评估TEER增加和减少的程度。因此可以考虑三类化合物。首先,其特征是TEER升高的时间很短,然后急剧下降(TEER50的值很高),其中包括perhexiline和异戊烯胺。毒性最高的化合物是第二种化合物,其特征在于TEER的变化最小,其中包括维拉帕米和地尔硫卓。该组与毒性较低的化合物有关,第三组以贝普利尔为代表,其特征在于依赖剂量的TEERmax和TEER50。因此,TEER测量似乎是比较抗钙剂毒性的一种非常简单的方法。

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