Carrier-Mediated Transport of H1-Antagonist at the Blood–Brain Barrier: Mepyramine Uptake into Bovine Brain Capillary Endothelial Cells in Primary Monolayer Cultures

Masahiro Yamazaki, Tetsuya Terasaki, Kuniaki Yoshioka, Osamu Nagata, Hideo Kato, Yasuo Ito, Akira Tsuji

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36 Citations (Scopus)

Abstract

The transport mechanism of the H1antagonist mepyramine at the blood-brain barrier (BBB) was studied by using primary cultured monolayers of bovine brain capillary endothelial cells (BCEC). The initial uptake of [3H]mepyramine into the BCEC showed strong temperature and concentration dependency, indicating that it involves both saturable and nonsaturable processes. Transport at the luminal membrane may be the rate-limiting process in the transcellular transport, since the values of the uptake coefficient of [3H]mepyramine at the luminal membrane (609 µl/mg protein/min) and the transcellular permeability coefficient (488 µl/mg protein/min) are very similar. The initial uptake of [3H]mepyramine was not affected by metabolic inhibitors, but was stimulated by preloading with the drug. Mepyramine appears to be transported into the BCEC by a carrier-mediated transport system which does not require metabolic energy, probably via a facilitated diffusion mechanism.

Original languageEnglish
Pages (from-to)975-978
Number of pages4
JournalPharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
Volume11
Issue number7
DOIs
Publication statusPublished - 1994 Jul

Keywords

  • H-antagonist
  • blood-brain barrier transport
  • carrier-mediated transport
  • mepyramine
  • primary cultured brain capillary endothelial cells

ASJC Scopus subject areas

  • Biotechnology
  • Molecular Medicine
  • Pharmacology
  • Pharmaceutical Science
  • Organic Chemistry
  • Pharmacology (medical)

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