Reversal of Multidrug Resistance in Human Leukemia K562 by Tamolarizine, a Novel Calcium Antagonist

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Author(s)

Abstract

A new type of organic Ca<SUP>2+</SUP> channel blocker, tamolarizine, was examined for its reversing effect on multidrug-resistant tumor cells.Tamolarizine synergistically potentiated the cytotoxicity of doxorubicin for doxorubicin-resistant K562 cells(K562/DXR)at a concentration of 0.1-10μM, but had hardly any synergistic effects in the parental cell line(K562)at the same concentration.Moreover, tamolarizine inhibits the P-glycoprotein pump-efflux activity in a dose-related manner and reduces the expression of the immunoreactive P-glycoprotein in K562/DXR cells as evaluated by cytofluorimetric assay.These results indicate that tamolarizine reverses the multidrug-resistance phenotype through direct interaction with P-gylcoprotein.

Journal

  • The Japanese Journal of Pharmacology

    The Japanese Journal of Pharmacology 82(3), 265-268, 2000-03-01

    The Japanese Pharmacological Society

References:  15

Codes

  • NII Article ID (NAID)
    10008183653
  • NII NACSIS-CAT ID (NCID)
    AA00691188
  • Text Lang
    ENG
  • Article Type
    SHO
  • ISSN
    00215198
  • NDL Article ID
    5321105
  • NDL Source Classification
    ZS51(科学技術--薬学)
  • NDL Call No.
    Z53-D199
  • Data Source
    CJP  NDL  J-STAGE 
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