P-glycoprotein as the drug efflux pump in primary cultured bovine brain capillary endothelial cells

Akira Tsuji, Tetsuya Terasaki, Yasushi Takabatake, Yoshiyuki Tenda, Ikumi Tamai, Tetsumori Yamashima, Shuzo Moritani, Takashi Tsuruo, Junkoh Yamashita

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288 Citations (Scopus)


The expression of a functional P-glycoprotein (P-gp) which pumps drugs out of brain capillary endothelial cells (BCEC) into blood was studied by evaluating the steady-state uptake and efflux of vincristine (VCR) by primary cultured bovine BCEC. The steady-state uptake of VCR was increased in the presence of metabolic inhibitors, and an anti-P-gp monoclonal antibody, MRK16, as well as verapamil and steroid hormones which are known to reverse multidrug resistance in tumor cells. Furthermore, efflux of VCR from BCEC was inhibited by verapamil. By immunohistochemistry, P-gp was localized at the luminal side of the capillary endothelial cells in both gray matter of bovine brain and primary cultured BCEC. These data suggest that P-gp functions as a drug efflux pump at the luminal side of BCEC and regulates the transfer of certain lipophilic drugs from the blood into the brain.

Original languageEnglish
Pages (from-to)1427-1437
Number of pages11
JournalLife Sciences
Issue number18
Publication statusPublished - 1992

ASJC Scopus subject areas

  • Biochemistry, Genetics and Molecular Biology(all)
  • Pharmacology, Toxicology and Pharmaceutics(all)


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