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首页> 外文期刊>The Journal of Clinical Pharmacology: Official Journal of the American College of Clinical Pharmacology >Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir.
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Fexofenadine transport in Caco-2 cells: inhibition with verapamil and ritonavir.

机译：非索非那定在Caco-2细胞中的转运：维拉帕米和利托那韦的抑制作用。

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This study investigated fexofenadine (FXD) transport and the inhibition of FXD transport in Caco-2 cell monolayer transwells, using rhodamine 123 (RH123) transport as a positive control. FXD transport from the basolateral (B) to apical (A) compartment was fivefold higher than A to B transport. FXD transport was linear with respect to time (up to 270 min) and concentration (up to 300 microm). Similar results were seen with the positive control RH123. Ritonavir (100 PM) and verapamil (100 microm) reduced transport of FXD and RH123 by more than 80%, whereas transport was not inhibited by 100 m indomethacin or 2 mM probenecid. This suggests predominantly P-glycoprotein (P-gp)-mediated transport as opposed to transport by multidrug resistance protein. In concentration-response experiments, FXD transport was inhibited by verapamil and ritonavir with IC50 values of 6.5 microm and 5.4 microm, respectively. Results from this in vitro study demonstrate differential transport of FXD across Caco-2 cell monolayers and inhibition of FXD transport by established P-gp inhibitors. Thefindings support the use of FXD as an index or probe compound to reflect P-gp activity in vivo.
机译：这项研究使用罗丹明123（RH123）转运作为阳性对照，研究了Fexofenadine（FXD）转运和FXD转运在Caco-2细胞单层穿孔中的抑制作用。从基底外侧（B）到顶端（A）隔室的FXD传输比从A到B的传输高五倍。 FXD转运相对于时间（最多270分钟）和浓度（最多300微米）呈线性关系。阳性对照RH123观察到相似的结果。利托那韦（100 PM）和维拉帕米（100微米）使FXD和RH123的转运减少了80％以上，而100 m消炎痛或2 mM丙磺舒未抑制转运。这表明与多药抗性蛋白的转运相反，P-糖蛋白（P-gp）介导的转运是主要的。在浓度响应实验中，维拉帕米和利托那韦抑制了FXD转运，IC50值分别为6.5微米和5.4微米。这项体外研究的结果表明，FXD跨Caco-2细胞单层的差异转运以及已建立的P-gp抑制剂对FXD转运的抑制作用。这些发现支持将FXD用作反映体内P-gp活性的指标或探针化合物。

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