Biochemical Pharmacology volume 78, issue 6, P642-647 2009 DOI: 10.1016/j.bcp.2009.05.026 View full text
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Cuyue Tang, Yuhsin Kuo, Nicole T. Pudvah, Joan D. Ellis, Maria S. Michener, Melissa Egbertson, Samuel L. Graham, Jacquelynn J. Cook, Jerome H. Hochman, Thomayant Prueksaritanont

Abstract: Brain penetration of drugs which are subject to P-glycoprotein (Pgp)-mediated efflux is attenuated, as manifested by the fact that the cerebrospinal fluid concentration (C(CSF)), a good surrogate of the unbound brain concentration (C(ub)), is lower than the unbound plasma concentration (C(up)) for Pgp substrates. In rodents, the attenuation magnitude of brain penetration by Pgp-mediated efflux has been estimated by correlating the ratio of CSF to plasma exposures (C(CSF)/C(p)) with the unbound fraction in plas…

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