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Aim:To investigate the modulatory effect of CJZ3,a lomerizine derivative,onP-glycoprotein(P-gp)function in rat brain microvessel endothelial cells(RBMEC).Methods:RBMEC were isolated and cultured in Dulbecco’s modified Eagle’s me-dium/F12(1:1)medium,and the amount of intracellular rhodamine 123(Rh 123)wasdetermined using a fluorescence spectrophotometer to evaluate the modulatoryeffect of CJZ3 on P-gp function.Results:The accumulation of Rh 123 was poten-tiated in a concentration-dependent manner after incubation with CJZ3 for RBMEC,but not for human umbilical vein endothelial cells(HUVEC).CJZ3 caused theaccumulation of intracellular Rh123 in a time-dependent manner and significantlydecreased the effiux of Rh 123 from the cells.The inhibitory effect of CJZ3 on P-gpfunction was reversible and remained for 120 min after CJZ3(2.5 μmol/L)wasremoved from the medium.Conclusion:CJZ3 has a potent in vitro effect on theinhibition of P-gp function.
Aim: To investigate the modulatory effect of CJZ3, a lomerizine derivative, onP-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). Methods: RBMEC were isolated and cultured in Dulbecco’s modified Eagle’s me- dium / F12 1: 1) medium, and the amount of intracellular rhodamine 123 (Rh 123) was determined using a fluorescence spectrophotometer to evaluate the modulatory effect of CJZ3 on P-gp function. Results: The accumulation of Rh 123 was poten- tiated in a concentration-dependent manner after incubation with CJZ3 for RBMEC, but not for human umbilical vein endothelial cells (HUVEC) .CJZ3 caused the accumulation of intracellular Rh123 in a time-dependent manner and significantly decreased the effiux of Rh 123 from the cells. inhibitory effect of CJZ3 on P -gpfunction was reversible and remained for 120 min after CJZ3 (2.5 μmol / L) was removed from the medium. Confluence: CJZ3 has a potent in vitro effect on the inhibition of P-gp function.