Damper D, Patton C L
J Protozool. 1976 May;23(2):349-56. doi: 10.1111/j.1550-7408.1976.tb03787.x.
Sensitivity to pentamidine of bloodstream forms and culture forms of Trypanosoma brucei brucei, strains of this subspecies, and strains of T. brucei rhodesiense characteristically differs in vitro. Analyses of transport parameters for pentamidine uptake in these organisms show differences that correspond with drug sensitivity. Long slender bloodstream forms of T. b. brucei have a high affinity for the drug and high rates of uptake at indicated by Km and Vmax values for [3H]pentamidine transport. Although pentamidine and stilbamidine resistance is associated with dyskinetoplasty, this condition does not itself confer resistance to pentamidine nor does it affect pentamidine transport. However, drug-resistant strains show lower rates for pentamidine transport as does T. b. rhodesiense, which is characteristically less sensitive to the drug. Of all the forms and strains studied, procyclic trypomastigotes were least sensitive to pentamidine and had a remarkable ability to exclude the drug.
布氏布氏锥虫的血流形式和培养形式、该亚种的菌株以及罗德西亚布氏锥虫的菌株对喷他脒的敏感性在体外存在特征性差异。对这些生物体中喷他脒摄取转运参数的分析显示出与药物敏感性相对应的差异。布氏布氏锥虫的长细血流形式对该药物具有高亲和力，并且如[3H]喷他脒转运的Km和Vmax值所示，摄取速率很高。虽然喷他脒和司替巴脒抗性与动基体发育不全有关，但这种情况本身并不赋予对喷他脒的抗性，也不影响喷他脒的转运。然而，耐药菌株的喷他脒转运速率较低，罗德西亚布氏锥虫也是如此，其对该药物的敏感性通常较低。在所有研究的形式和菌株中，前循环型锥鞭毛虫对喷他脒最不敏感，并且具有显著的排除该药物的能力。
