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Wiley InterScience | |||||
  Acta Pharmacologica SinicaVolume 26 Issue 2, Pages 166 - 170 Published Online: 27 Jan 2005 © 2008 CPS and SIMM Official journal of the Chinese Pharmacological Society and Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract | References | Full Text: PDF (Size: 418K) | Related Articles | Citation Tracking  Modulation of P-glycoprotein function by amlodipine derivatives in brain microvessel endothelial cells of rats Copyright 2005 CPS and SIMM KEYWORDS amlodipine derivatives • CJX1 • CJX2 • verapamil • P-glycoprotein • blood brain barrier • vascular endothelium Abstract
Aim: To investigate whether the amlodipine derivatives, CJX1 and CJX2, have a modulative effect on P-glycoprotein (P-gp) function in rat brain microvessel endothelial cells (RBMEC). Methods: Isolated RBMEC were cultured in DMEM/F12 (1:1) medium. The amount of intracellular rhodamine (Rh123) was determined, using a fluorescence spectrophotometer, to evaluate the function of P-gp. Results: The accumulation of Rh123 in RBMEC was potentiated in a concentration dependent manner after incubation with CJX1 and CJX2 at 1, 2.5, 5, and 10 μmol/L (P<0.01), but no accumulation of Rh123 was observed in human umbilical vein endothelial cells after incubation with CJX1 and CJX2 10 μmol/L (P>0.05). Accumulation of intracellular Rh123 was increased and efflux of intracellular Rh123 was decreased in a time-dependent manner from 0–100 min after CJX1 and CXJ2 at 10 μmol/L treatment. The inhibitory effect of CJX1 and CJX2 on P-gp function was reversible and remained even at 120 min after removal of CJX1 and CJX2 at 2.5 μmol/L from the medium. Conclusion: CJX1 and CJX2 exhibited a potent effect in the inhibition of P-gp function in vitro. Received 2004-06-11 Accepted 2004-11-08 | 
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