Sutherland I A, Holmes P H
Department of Zoology, University of Aberdeen, UK.
Acta Trop. 1993 Sep;54(3-4):271-8. doi: 10.1016/0001-706x(93)90099-w.
The transport of isometamidium chloride (Samorin) in Trypanosoma congolense which were either sensitive or resistant to this widely used trypanocide was studied in vitro. Significantly lower amounts of drug were accumulated over time by resistant than by sensitive trypanosomes. While no direct evidence could be obtained, indirect observations implied the involvement of an increased efflux of drug from the resistant trypanosomes. In both the resistant and sensitive parasites, drug transport was found to be mediated by an energy-dependent, specific process, presumably receptor-mediated. However, the specificity of the putative receptors was altered in the drug-resistant parasites. It is proposed that an alteration or replacement of a specific receptor in isometamidium chloride-resistant T. congolense results in an increased efflux of the drug and that this increased efflux at least partially mediates the reduction in sensitivity to the compound.
在体外研究了异美啶氯化物（沙莫林）在对这种广泛使用的杀锥虫剂敏感或耐药的刚果锥虫中的转运情况。随着时间的推移，耐药锥虫积累的药物量明显低于敏感锥虫。虽然无法获得直接证据，但间接观察表明耐药锥虫中药物外排增加。在耐药和敏感寄生虫中，均发现药物转运是由能量依赖性的特定过程介导的，推测是受体介导的。然而，在耐药寄生虫中，假定受体的特异性发生了改变。有人提出，在对异美啶氯化物耐药的刚果锥虫中，特定受体的改变或替换导致药物外排增加，并且这种增加的外排至少部分介导了对该化合物敏感性的降低。
