The Japanese Journal of Pharmacology
Online ISSN : 1347-3506
Print ISSN : 0021-5198
ISSN-L : 0021-5198
Short Communications
Reversal of Multidrug Resistance in Human Leukemia K562 by Tamolarizine, a Novel Calcium Antagonist
Norihisa MiyakeRyousuke FujitaMasaaki IshikawaMotoaki TakayanagiYoshio TakayanagiKen-ichi Sasaki
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2000 年 82 巻 3 号 p. 265-268

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A new type of organic Ca2+ 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.
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© The Japanese Pharmacological Society 2000
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