Summary
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.
Résumé
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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Barrand, M.A., Robertson, K., von Weikersthal, S.F., Horwell, D. (1996). Peptide-Like Drugs May be Excluded from the Brain by P-Glycoprotein at the Blood-Brain Barrier. In: Couraud, PO., Scherman, D. (eds) Biology and Physiology of the Blood-Brain Barrier. Advances in Behavioral Biology, vol 46. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-9489-2_34
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DOI: https://doi.org/10.1007/978-1-4757-9489-2_34
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