Application of a high-resolution in vitro human MDR1-MDCK assay and in vivo studies in preclinical species to improve prediction of CNS drug penetration.

Although the CSF Kp,uu showed a trend of overestimating brain Kp,uu of MDR1 substrates, the CSF Kp,uu were generally in a good agreement with brain Kp,uu (within 3‐fold) except for two MDR1 substrates, compounds 6 and 7, which had very high protein binding with fu,p < 0.01 and very low brain Kp,uu.

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