Abstract:Background Blood-brain barrier permeability (BBB Pe) and unbound brain-to-plasma concentration ratio (Kp,uu,brain) are relevant parameters describing the brain uptake potential of compounds. BBB efflux by transporter proteins, mainly MDR-1 and BCRP, is an essential factor determining Kp,uu,brain. Kp,uu,brain-values are commonly estimated in vivo in rats and monkeys and predicted using in silico methodology. Such estimates can be used to predict corresponding human clinical values. Objective The objective of th… Show more
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