Peters W, Robinson B L, Mittelholzer M L, Crevoisier C, Stürchler D
CABI International Institute of Parasitology, St Albans, U.K.
Ann Trop Med Parasitol. 1995 Oct;89(5):465-8. doi: 10.1080/00034983.1995.11812978.
A comparison was made between the blood schizontocidal action in mice of racemic mefloquine hydrochloride and the free bases of its (+)- and (-)-enantiomers (Ro 13-7224 and Ro 13-7225) against chloroquine-resistant Plasmodium yoelii ssp. NS. The racemic hydrochloride was two to three times as active against this parasite in mice as either of the enantiomer free bases, which were of similar activity to each other. Under drug selection pressure, the parasites acquired resistance in approximately the same time for each of the three compounds.
对盐酸消旋甲氟喹及其(+)-和(-)-对映体(Ro 13-7224和Ro 13-7225)游离碱对氯喹抗性约氏疟原虫ssp. NS的小鼠血液裂殖体杀灭作用进行了比较。盐酸消旋体对该寄生虫在小鼠体内的活性是两种对映体游离碱中任何一种的两到三倍,而这两种对映体游离碱的活性彼此相似。在药物选择压力下,三种化合物中的每一种使寄生虫产生耐药性的时间大致相同。