Biochemical Pharmacology volume 78, issue 6, P642-647 2009 DOI: 10.1016/j.bcp.2009.05.026 View full text
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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