[Reversal of multidrug resistance with (R)-verapamil in vitro and in vivo].
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.
Pommerenke
E W
EW
Institut für Experimentelle Pathologie, Deutschen Krebsforschungszentrums Heidelberg.
Mattern
J
J
Traugott
U
U
Volm
M
M
D000818:Animals; D000970:Antineoplastic Agents / Q000494:pharmacology*; D003561:Cytarabine / Q000494:pharmacology; D004317:Doxorubicin / Q000494:pharmacology; D004351:Drug Resistance; D005260:Female; D007939:Leukemia L1210 / Q000188:drug therapy; D051379:Mice; D013237:Stereoisomerism; D013936:Thymidine / Q000031:analogs & derivatives / Q000378:metabolism; D014407:Tumor Cells, Cultured / Q000187:drug effects; D014529:Uridine / Q000378:metabolism; D014700:Verapamil / Q000494:pharmacology*
D000970:Antineoplastic Agents; D003561:Cytarabine; D004317:Doxorubicin; C012439:methylthymidine; D014700:Verapamil; D013936:Thymidine; D014529:Uridine
Durchbrechung der Multidrug-Resistenz mit (R)-Verapamil in vitro und in vivo.