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

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.

journal_name

Acta Pharmacol Sin

journal_title

Acta pharmacologica Sinica

authors

Ji BS,He L,Li XQ,Liu GQ

doi

10.1111/j.1745-7254.2006.00294.x

subject

Has Abstract

pub_date

2006-04-01 00:00:00

pages

414-8

issue

4

eissn

1671-4083

issn

1745-7254

journal_volume

27

pub_type

杂志文章

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