In vitro assessment of drug candidates' ability to cross the blood-brain barrier, identifying P-glycoprotein interactions.
In vitro MDR1-MDCKII permeability assays areused to assess the ability of drug candidates to cross the blood-brain barrier (BBB) and to identify P-glycoprotein (P-gp) substrates and inhibitors.MDR1-MDCKII cells, which express the human P-gp protein, are grown on semi-permeable supports and used in a dual-chamber diffusion system to simulate the BBB.The assay helps determine the apparent permeability coefficient (Papp) and efflux ratios, which can be used to predict brain penetration and identify potential drug interactions with P-gp.
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Nick Lynch (2025) studied this question.
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