Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers

Abstract

Abstract: AIM: To study the effect of Lomerizine on the activity of P-glycoprotein (P-gp)in the bloodbrain barrier(BBB)and search for novel effective P-gPinhibiting agent against multidrug resistance.METHODS: Rhodamine123 (Rh123)was used to examine the activity of P-gPand RT-PCR to study the mdr mRNA expression in cultured rat brain microvessel endothelial cells (RBMECs).RESULTS: Lomerizine could increase the cellular Rh123 in RBMECs in a concentration-dependent manner.RT-PCR indicated that lomerizine could not down-regulate the expression of mdr mRNA.CONCLUSION: Lomerizine can reverse multidrug resistance in the blood-brain barrier by inhibiting the activity of P-gp.

Key words: lomerizine, P-glycoprotein, bloodbrain barrier, RT-PCR

CLC Number:

R965.2
R966

LI Yun-man, KANG Kai, FANG Wei-rong. Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2006, 11(10): 1110-1114.

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