Abstract:Recent advances in our knowledge of the blood–brain barrier (BBB) have in part been made by studying the properties and function of cerebral endothelial cells in vitro. After an era of working with a fraction, enriched in cerebral microvessels by centrifugation, the next generation of in vitro BBB model systems was introduced, when the conditions for routinely culturing the endothelial cells were established. This review summarizes the results obtained from this rapidly growing field. It can be stated with certainty that, in addition to providing a better insight into the chemical composition of cerebral endothelial cells, much has been learned from these studies about the characteristics of transport processes and cell‐to‐cell interactions during the last 12 years. With the application of new technologies, the approach offers a new means of investigation, applicable not only to biochemistry and physiology but also to the drug research, and may improve the transport of substances through the BBB. The in vitro approach has been and should remain an excellent model of the BBB to help unravel the complex molecular interactions underlying and regulating the permeability of the cerebral endoth