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  • Title: [Blood plasma proteins and drug transport across the hemato-encephalic barrier].
    Author: Lutsevich AN, Bender KI, Kupchikov VV.
    Journal: Farmakol Toksikol; 1991; 54(1):70-6. PubMed ID: 1860509.
    Abstract:
    The blood-brain barrier being a dynamic membrane interface between the blood and the brain is of great importance for the formation of the pharmacokinetics and pharmacodynamics of neurotropic drugs. One of the main factors influencing diffusion of drugs into the central nervous system is the degree of their binding by plasma proteins. It was supposed that only the unbound fraction of drugs is pharmacologically active. However in some papers the plasma-protein-mediated transport into the rat brain of endogenous compounds and drugs was demonstrated. This indicates that the measuring of the free fraction of a drug in vitro can lead to the underestimation of its concentration in the target organ.
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