REVERSAL OF MULTIDRUG-RESISTANCE IN MURINE FIBROSARCOMA CELLS BY THIOXANTHENE FLUPENTIXOL

被引：24

作者：

FAN, D ^{[1
]}

POSTE, G ^{[1
]}

SEID, C ^{[1
]}

EARNEST, LE ^{[1
]}

BULL, T ^{[1
]}

CLYNE, RK ^{[1
]}

FIDLER, IJ ^{[1
]}

机构：

[1] SMITHKLINE BEECHAM PHARMACEUT,RES & DEV,KING OF PRUSSIA,PA 19406

来源：

INVESTIGATIONAL NEW DRUGS | 1994年 / 12卷 / 03期

关键词：

MULTIDRUG RESISTANCE; FLUPENTIXOL; CHEMOSENSITIZATION; P-GLYCOPROTEIN;

D O I：

10.1007/BF00873959

中图分类号：

R73 [肿瘤学];

学科分类号：

100214 ;

摘要：

The purpose of this study was to identify calcium channel and calmodulin antagonists effective in increasing the cytotoxic effects of several chemotherapeutic drugs against UV-2237 murine fibrosarcoma MDR cells. Among 8 compounds tested at nontoxic concentrations, flupentixol, a piperazine-substituted thioxanthene, was the most potent in enhancing the cytotoxicity of anticancer drugs commonly associated with the multidrug resistant (MDR) phenotype, such as Adriamycin, actinomycin D, vinblastine, and vincristine, but not 5-fluorouracil, a drug usually unaffected by MDR. The chemosensitizing effects of flupentixol were produced by increasing intracellular drug accumulation via a mechanism unrelated to the binding of the plasma membrane P-glycoprotein.

引用

页码：185 / 195

页数：11

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