Tapiero H, Fourcade A, Munck J N, Zwingelstein G, Lampidis T J
Drugs Exp Clin Res. 1986;12(1-3):265-73.
Adriamycin-resistant cells express a multiple drug resistance phenotype characterized by cross-resistance to compounds of related and unrelated structure and action. The pharmacological determinants of this resistance, such as decreased drug uptake and/or decreased drug retention, are associated with biochemical alterations in the cells. To overcome multiple drug resistance, a calcium-channel blocking agent, verapamil, was used, which acted by increasing the amount of drug retained in resistant cells and consequently enhanced the cytotoxic effectiveness. The basis for this enhanced retention and cytotoxicity is not known. Whether these compounds sensitize the cells to the action of, or potentiate the effect of, anticancer drugs remains to be determined. The preliminary data tend to support the second possibility.
阿霉素耐药细胞表现出多药耐药表型，其特征为对结构和作用相关及不相关的化合物产生交叉耐药。这种耐药的药理学决定因素，如药物摄取减少和/或药物滞留减少，与细胞中的生化改变有关。为了克服多药耐药，使用了一种钙通道阻滞剂维拉帕米，它通过增加耐药细胞中滞留的药量起作用，从而增强细胞毒性效果。这种增强的滞留和细胞毒性的基础尚不清楚。这些化合物是使细胞对抗癌药物的作用敏感，还是增强抗癌药物的效果，仍有待确定。初步数据倾向于支持第二种可能性。
