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(R)-维拉帕米在体内外逆转多药耐药性

[Reversal of multidrug resistance with (R)-verapamil in vitro and in vivo].

作者信息

Pommerenke E W, Mattern J, Traugott U, Volm M

机构信息

Institut für Experimentelle Pathologie, Deutschen Krebsforschungszentrums Heidelberg.

出版信息

Arzneimittelforschung. 1991 Aug;41(8):855-8.

PMID:1781810
Abstract

The clinical use of racemic (R/S)-verapamil (CAS 52-53-9) as resistance modifier is limited because of the cardiovascular activity of the substance. The stereoisomer (R)-verapamil shows significant less cardiovascular activity. Therefore we tested the resistance modifying abilities of (R)-verapamil and (R/S)-verapamil in murine multidrug-resistant L 1210 ascites-tumor-cells in vitro and in vivo. The present results demonstrate, that the (R)-isomer has the same resistance modifying effects as racemic verapamil. Both modifying substances have no effects in the parental (sensitive) and cytosine-arabinoside resistant L 1210 ascites-tumor-cells. Thus, (R/S)-verapamil and (R)-verapamil show their resistance modifying abilities only in multidrug-resistant tumor-cells.

摘要

消旋(R/S)-维拉帕米(CAS 52-53-9)作为耐药修饰剂的临床应用因该物质的心血管活性而受到限制。立体异构体(R)-维拉帕米的心血管活性明显较低。因此,我们在体外和体内对小鼠多药耐药L 1210腹水肿瘤细胞测试了(R)-维拉帕米和(R/S)-维拉帕米的耐药修饰能力。目前的结果表明,(R)-异构体具有与消旋维拉帕米相同的耐药修饰作用。两种修饰物质对亲代(敏感)和阿糖胞苷耐药的L 1210腹水肿瘤细胞均无作用。因此,(R/S)-维拉帕米和(R)-维拉帕米仅在多药耐药肿瘤细胞中显示出它们的耐药修饰能力。

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