Despite their structural similarity, the two anti-influenza adamantane compounds amantadine (AMA) and rimantadine (RIM) exhibit strikingly different rates of blooda??brain barrier (BBB) transport. However, the molecular mechanisms facilitating the higher rate of in situ BBB transport of RIM, relative to AMA, remain unclear. The aim of this study, therefore, was to determine whether differences in the extent of brain uptake between these two adamantanes also occurred in vivo, and elucidate the potential carrier protein facilitating their BBB transport using immortalized human brain endothelial cells (hCMEC/D3).
Kooijmans, S. A. A., Senyschyn, D., Mezhiselvam, M. M., Morizzi, J., Charman, S. A., Weksler, B., ... Nicolazzo, J. (2012). The involvement of a Na+ - and Cl- -dependent transporter in the brain uptake of amantadine and rimantadine. Molecular Pharmaceutics, 9, 883 - 893. https://doi.org/10.1021/mp2004127