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替阿帕米类似物DMDP对阿霉素耐药及敏感P388细胞中阿霉素外排的影响。

Effects of DMDP, a tiapamil analogue, on adriamycin efflux in adriamycin-resistant and -sensitive P388 cells.

作者信息

Radel S, Mayhew E, Rustum Y M

机构信息

Department of Experimental Pathology, Roswell Park Memorial Institute, Buffalo, N.Y. 14263.

出版信息

Anticancer Res. 1987 Nov-Dec;7(6):1105-8.

PMID:3442407
Abstract

The calcium channel blockers 'DMDP' [N-3,4-dimethoxyphenethyl)-N-methyl-2-(2-naphthyl-m-dithane-2-prop ylamine)] and verapamil inhibited the active efflux of adriamycin from adriamycin-resistant P388 leukemia cells but had no effect on the drug-sensitive cell line. However, after removal of the calcium channel blockers, DMDP at a low drug concentration caused a much longer inhibition of this efflux pathway than verapamil. This may be attributed to the higher binding affinity of DMDP for receptor sites.

摘要

钙通道阻滞剂“DMDP”[N-(3,4-二甲氧基苯乙基)-N-甲基-2-(2-萘基间二硫戊环-2-丙胺)]和维拉帕米抑制了阿霉素从耐阿霉素的P388白血病细胞中的主动外排,但对药物敏感细胞系没有影响。然而,在去除钙通道阻滞剂后,低药物浓度的DMDP对这种外排途径的抑制作用比维拉帕米长得多。这可能归因于DMDP对受体位点的更高结合亲和力。

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