CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells.

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Ji BS, He L, Li XQ, Liu GQ

CJZ3, a lomerizine derivative, modulates P-glycoprotein function in rat brain microvessel endothelial cells.

Acta Pharmacol Sin. 2006 Apr;27(4):414-8. doi: 10.1111/j.1745-7254.2006.00294.x.

PubMed ID

16539840 [ View in PubMed

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Abstract

AIM: To investigate the modulatory effect of CJZ3, a lomerizine derivative, on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). METHODS: RBMEC were isolated and cultured in Dulbecco modified Eagle medium/F12 (1:1) medium, and the amount of intracellular rhodamine 123 (Rh123) was determined using a fluorescence spectrophotometer to evaluate the modulatory effect of CJZ3 on P-gp function. RESULTS: The accumulation of Rh123 was potentiated 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 efflux of Rh123 from the cells. The inhibitory effect of CJZ3 on P-gp function was reversible and remained for 120 min after CJZ3 (2.5 micromol/L) was removed from the medium. CONCLUSION: CJZ3 has a potent in vitro effect on the inhibition of P-gp function.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Lomerizine	P-glycoprotein 1	Protein	Humans	Yes	Inhibitor	Details