Aim:To investigate the characteristics of carbamazepine(CBZ)transport anddrug interactions at the blood-brain barrier.Methods:Cultured rat brain microvas-cular endothelial cells(rBMEC)were used as an in vitro model of the blood-brainbarrier(BBB).When cells became confluent,CBZ uptake over time was recordedby incubation of the cells in a medium containing 10 mg/L CBZ at 37℃.Thesteady-state uptake of CBZ by rBMEC was tested for different CBZ concentra-tions at 37℃.The effects of various agents on the steady-state uptake of CBZand efflux of CBZ from rBMEC were also studied.Results:The uptake of CBZ byrBMEC was time-and concentration-dependent.The steady-state uptake oc-curred at 30 rain for incubation.The steady-state uptake was significantly in-creased(P<0.01)by treatment with dinitrophenol.The co-administration ofcyclosporine A significantly increased the steady-state uptake of CBZ by therBMEC,whereas co-administration of olanzapine significantly decreased the up-take in a concentration-and temperature-dependent manner.The efflux of CBZfrom rBMEC was inhibited by CsA.Conclusion:The transport of CBZ at the BBBis mediated by many transporters.Some specific ABC(ATP-binding cassette,ABC)efflux transporters may be involved in the transport of CBZ.Drugs influ-ence the transport of CBZ at the BBB in different ways. Aim: To investigate the characteristics of carbamazepine (CBZ) transport and drug interactions at the blood-brain barrier. Methods: Cultured rat brain microvas-cular endothelial cells (rBMEC) were used as an in vitro model of the blood-brain barrier (BBB). The cells became confluent, CBZ uptake over time was recorded in incubation of the cells in a medium containing 10 mg / L CBZ at 37 ° C. The Tensteady-state uptake of CBZ by rBMEC was tested for different CBZ concentra- tions at 37 ° C. The effects of various agents on the steady-state uptake of CBZ and efflux of CBZ from rBMEC also studied. Results: The uptake of CBZ byrBMEC was time-and concentration-dependent.The steady-state uptake oc-curred at 30 rain for incubation. steady-state uptake was significantly in-creased (P <0.01) by treatment with dinitrophenol.The co-administration ofcyclosporine A significantly increased the steady-state uptake of CBZ by therBMEC, yet co-administration of olanzapine significantly decreased the up-take in a concentra tion-and temperature-dependent manner.The efflux of CBZfrom rBMEC was inhibited by CsA.Conclusion: The transport of CBZ at the BBB mediated mediated by many transporters.Some specific ABC (ATP-binding cassette, ABC) efflux transporters may be involved in the transport of CBZ.Drugs influ-ence the transport of CBZ at the BBB in different ways.