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- W1469353282 abstract "Many tools are used to provide data for blood-brain barrier (BBB) permeability, brain exposure, and unbound blood to brain distribution. The data are used to guide brain exposure optimization, develop pharmacokinetic-pharmacodynamic relationships, and plan clinical studies. Peripheral drug discovery teams use the data to guide BBB permeation reduction to minimize central nervous system side effects. Passive transcellular diffusion BBB permeability ( P app ) is assessed computationally using log P and topological polar surface area and in vitro using parallel artificial membrane permeability assay-blood-brain barrier, Δlog P , immobilized artificial membrane, high-performance liquid chromatography, and Madin-Darby canine kidney cell monolayer permeability. Efflux ratio is assessed using in vitro MDR1 (multidrug resistant protein 1)-MDCKII (and other cell lines transfected with specific human BBB efflux transporter genes) and Caco-2, and in vivo using mouse strains knocked out for specific BBB efflux transporters. in vivo neuroPK studies provide an array of BBB permeability, transporter effects, brain exposure data ( C bu , AUC bu ), and unbound brain to blood partition coefficient ( K puu ). Brain binding studies, using equilibrium dialysis of brain homogenate or brain slice method, provide f ub , which is used to convert in vivo total brain concentration to C bu . Microdialysis and cerebrospinal fluid (CSF) sampling in vivo directly measure C bu and CSF concentration." @default.
- W1469353282 created "2016-06-24" @default.
- W1469353282 creator A5015723806 @default.
- W1469353282 creator A5018505975 @default.
- W1469353282 date "2016-01-01" @default.
- W1469353282 modified "2023-10-16" @default.
- W1469353282 title "Blood-Brain Barrier Methods" @default.
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