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Table 3 In vivo Göttingen minipig Kp,uu,brain (from previous publication [20],) and in vitro Kp,uu,brain from Uni-L calculated with use of predicted (Pre.fu) and determined (Det.fu) fu data

From: Application of a new MDCKII-MDR1 cell model to measure the extent of drug distribution in vitro at equilibrium for prediction of in vivo unbound brain-to-plasma drug distribution

  1. The brain penetration classification is shown in three colours for compounds (n = 12): restricted (Kp,uu,brain < 0.3) in orange, partially restricted (Kp,uu,brain between 0.3 and 0.7) in yellow, and unrestricted (Kp,uu,brain > 0.7) in green. In a separate column is the Efflux ratio demonstrated from a conventional transport study (also captured in Table 1). Compounds considered to be uptake substrates have been excluded (metoclopramide, doxepin, diphenhydramine, and fluoxetine)
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Fluids and Barriers of the CNS

ISSN: 2045-8118