Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction.

@article{Summerfield2007CentralNS,
  title={Central nervous system drug disposition: the relationship between in situ brain permeability and brain free fraction.},
  author={Scott G. Summerfield and Kevin Read and David J. Begley and T. Obradovic and Ismael J. Hidalgo and Sara A Coggon and A. V. Lewis and Rod A. Porter and Phil Jeffrey},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2007},
  volume={322 1},
  pages={205-13}
}
The dispositions of 50 marketed central nervous system (CNS) drugs into the brain have been examined in terms of their rat in situ (P) and in vitro apparent membrane permeability (P(app)) alongside lipophilicity and free fraction in rat brain tissue. The inter-relationship between these parameters highlights that both permeability and brain tissue binding influence the uptake of drugs into the CNS. Hydrophilic compounds characterized by low brain tissue binding display a strong correlation (R(2… CONTINUE READING
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