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 


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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