Peptide-Like Drugs May be Excluded from the Brain by P-Glycoprotein at the Blood-Brain Barrier

  • M. A. Barrand
  • K. Robertson
  • S. F. von Weikersthal
  • D. Horwell
Part of the Advances in Behavioral Biology book series (ABBI, volume 46)


Peptide-like compounds, particularly a NK1 antagonist and to a small extent CCKA and CCKB antagonists, appear to interact with P-glycoprotein since they show effects on intracellular drug accumulation and can displace photoaffinity labelling of the protein. They may thus be P-glycoprotein substrates, liable to expulsion from the blood-brain-barrier.


Cyclic Peptide Photoaffinity Labelling Drug Efflux Transporter Intracellular Drug Accumulation Peptide Receptor Antagonist 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.


Quelques composés de type peptidique, en particulier un antagoniste du récepteur NK1, et à un moindre degré des antagonistes des récepteurs CCKA et CCKB, semblent interagir avec la P-gp, puisqu’ils agissent sur l’accumulation intracellulaire de médicaments et peuvent déplacer le photomarquage de la protéine. Ils peuvent donc être considérés comme des substrats de la P-gp, susceptibles d’être expulsés de la BHE.


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Copyright information

© Springer Science+Business Media New York 1996

Authors and Affiliations

  • M. A. Barrand
    • 1
  • K. Robertson
    • 1
  • S. F. von Weikersthal
    • 1
  • D. Horwell
    • 2
  1. 1.Department of PharmacologyUniversity of CambridgeCambridgeUK
  2. 2.Department of Chemistry Parke-Davis ResearchAddenbrooke’s Hospital SiteCambridgeUK

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