Lomerizine inhibits activity of P-glycoprotein in primary cultured brain microvessel endothelial cell monolayers
- VernacularTitle:洛美利嗪抑制原代培养的脑微血管内皮细胞上P-糖蛋白的活性
- Author:
Yunman LI
;
Kai KANG
;
Weirong FANG
- Publication Type:Journal Article
- From:
Chinese Journal of Clinical Pharmacology and Therapeutics
2006;11(10):1110-1114
- CountryChina
- Language:Chinese
-
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-gp inhibiting agent against multidrug resistance. METH-ODS: Rhodamine123 (Rh123) was used to examine the activity of P-gp and 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. CONCLU-SION: 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
