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Differences between the Calculated Fraction Available for BBB Transport and the in Vitro Measured Free Fraction Could be Explained by Capillary Heterogeneity

  • C. Videbæk
  • P. Ott
  • O. B. Paulson
  • G. M. Knudsen
Part of the Advances in Behavioral Biology book series (ABBI, volume 46)

Summary

It has earlier been shown that presence of albumin in the brain capillaries apparently enhances uptake of protein bound substances (Pardridge and Fierer, J. Neurochem. 54: 971–976,1990; Pardridge and Landaw, Am. J. Physiol. 249: E5534–E542, 1985; Westphal Receptors and hormone action. Acad. Press 443–472, 1978; Jones et al. J. Pharmacol. Exp. Ther:, 245: 816–822, 1988; Cornford et al. J. Neurochem., 44: 1541–1550, 1985). This study evaluated the protein-ligand interaction for two benzodiazepine antagonists, iomazenil and flumazenil, in rats by comparaison of the calculated fraction available for BBB transport (favail) and the in vitro measured free fraction (feq).

Keywords

Cerebral Blood Flow Hormone Action Calculate Fraction Brain Capillary Paul Scherrer Institute 
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.

Résumé

Il a été montré précédemment que lorsque des substances sont fixées dans le sang à l’albumine, leur captation au niveau des capillaires cérébraux est augmentée (Pardridge and Fisher, J. Neurochem.,54:974–976, 1990; Pardridge and Landaw, Amer. J. Phvsiol.,249:534–E542,1985; Westphal Receptors and hormone action. Acad. Press 443–472, 1978; Jones et al., J. Pharmacol. Exp. Ther., 245:816–822, 1988; Cornford et al., J. Neurochem., 44:1541–1550, 1985). Nous avons évalué l’interaction de deux antagonistes de la benzodiazépine, l’iomazenil et leflumazenil à l’albumine et calculé la fraction libre disponible pour le transport à travers la BHE (flibre). Nous avons aussi mesuré cette fraction libre in vitro (feq).

Copyright information

© Springer Science+Business Media New York 1996

Authors and Affiliations

  • C. Videbæk
    • 1
  • P. Ott
    • 2
  • O. B. Paulson
    • 2
  • G. M. Knudsen
    • 2
  1. 1.Department of HepatologyState University Hospital RigshospitaletCopenhagenDenmark
  2. 2.Department of NeurologyState University Hospital RigshospitaletCopenhagenDenmark

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