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目的:研究P-糖蛋白(P-gp)是否限制尼莫地平(NMD)从血液循环进入脑内。方法:当原代培养的鼠脑微血管内皮细胞(BCEC)长至互相连接成片时,加入含有NMD 10mg/L的Hanks’液37℃温孵,记录细胞摄取NMD的时间过程,将含有NMD和各种不同受试药物的Hanks’液分别加入到不同培养孔中,检测90min时细胞对NMD的摄取量,在细胞摄取NMD 90min后,分别加入红霉素,克拉霉素和环孢素A以检测P-糖蛋白抑制剂对原代培养的脑微血管内皮细胞外排NMD的影响。结果:细胞对NMD的摄取呈时间依赖性,P-gp抑制剂或代谢抑制剂的加入会增加稳态时NMD在细胞内的浓度,P-gp抑制剂的加入也使NMD的外排受到了抑制。结论:P-gp限制NMD进入脑内,P-gp抑制剂的加入可增加NMD的进入。
PURPOSE: To investigate whether P-glycoprotein (P-gp) limits nimodipine (NMD) from circulating into the brain. Methods: When primary cultured rat brain microvascular endothelial cells (BCECs) grew into interconnected patches, Hanks’ solution containing NMD 10 mg / L was incubated at 37 ° C. The time course of NMD uptake was recorded and the cells containing NMD and Hanks’ solution of various drugs were added to different culture wells to detect the uptake of NMD by the cells at 90 min. After the cells were taken in for 90 min, erythromycin, clarithromycin and cyclosporine A To detect the effect of P-glycoprotein inhibitor on the NMD of primary cultured brain microvascular endothelial cells. Results: The cell uptake of NMD was time-dependent. The addition of P-gp inhibitor or metabolic inhibitor increased the intracellular concentration of NMD at homeostasis. The addition of P-gp inhibitor also affected the efflux of NMD inhibition. Conclusion: P-gp limits NMD entry into the brain. The addition of P-gp inhibitor may increase the entry of NMD.