Carrier-Mediated Transport of H1-Antagonist at the Blood-Brain Barrier: A Common Transport System of H1-Antagonists and Lipophilic Basic Drugs

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

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39 Citations (Scopus)


The blood-brain barrier (BBB) transport system for H1 antagonists was studied using primary cultured bovine brain capillary endothelial cells (BCEC). The uptake of [3H]mepyramine was inhibited by various H1-antagonists. Ketotifen competitively inhibited [3H]mepyramine uptake with an inhibition constant (Ki ) of 46.8 µM. Lipophilic basic drugs such as propranolol, lidocaine and imipramine significantly inhibited [3H]mepyramine uptake. In particular, propranolol inhibited [3H]mepyramine uptake competitively at an inhibition constant (Ki) of 51.1 µM. Moreover, in ATP-depleted BCEC, [3H]mepyramine uptake was stimulated by preloading with H1- antagonists and lipophilic basic drugs. These results indicated that H1-antagonists are transported across the BBB via a carrier-mediated transport system common to lipophilic basic drugs.

Original languageEnglish
Pages (from-to)1516-1518
Number of pages3
JournalPharmaceutical Research: An Official Journal of the American Association of Pharmaceutical Scientists
Issue number11
Publication statusPublished - 1994 Nov


  • H-antagonist
  • blood-brain barrier (BBB)
  • common transport system
  • lipophilic basic drugs
  • propranolol

ASJC Scopus subject areas

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

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