m-AMSA as a probe for transport phenomena associated with anthracycline resistance.
Kinetics of transport of the acridine derivative 4'-(9-acridinylamino)-methanesulfon-m-anisidide (m-AMSA) were examined in P388 murine leukemia cells and in P388/ADR, a subline selected for adriamycin resistance and cross-resistant to a variety of drugs including m-AMSA. Compared with the drug-responsive parent cell line, P388/ADR cells showed impaired accumulation of m-AMSA and an enhanced rate of drug exodus. Competition studies demonstrated structural specificity of the outward transport process. There was a low degree of intracellular m-AMSA binding, and steady-state drug levels were reached in less than 1 min. These results suggest that m-AMSA will be a useful probe for studying transport systems associated with anthracycline resistance.
D000585:Aminacrine / Q000031:analogs & derivatives / Q000378:metabolism*; D000609:Aminoacridines / Q000378:metabolism*; D000818:Animals; D000903:Antibiotics, Antineoplastic / Q000494:pharmacology*; D000970:Antineoplastic Agents / Q000378:metabolism*; D001692:Biological Transport; D002460:Cell Line; D004351:Drug Resistance; D007941:Leukemia P388 / Q000378:metabolism; D051379:Mice; D009279:Naphthacenes / Q000494:pharmacology
D000609:Aminoacridines; D000903:Antibiotics, Antineoplastic; D000970:Antineoplastic Agents; D009279:Naphthacenes; D000585:Aminacrine; C013389:4'-(9-acridinylamino)methanesulfonanilide