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甲氟喹盐酸盐-mefloquine(WR 142,490)是一个4-喹啉甲醇类的新衍生物,它的化学名称为α-(-2哌啶)-2,8-双三氟甲基-4-喹啉甲醇。30年前已发现一些4-喹啉甲醇类化合物在鸟疟模型表现出抗疟作用。其中,SN10,275对人间日疟具有长效杀血裂殖体作用,但由于光毒毒性而不能广泛使用。WR30,090对氯喹敏感株或抗性株恶性疟原虫均有高效,光毒毒性最小,但杀血裂殖体作用的时间相当短。甲氟喹经临床前研究表明比WR30,090
Mefloquine hydrochloride - mefloquine (WR 142,490) is a novel derivative of 4-quinolinemethanol whose chemical name is α - (-2piperidine) -2,8-bistrifluoromethyl-4 - quinoline methanol. Some 4-quinolinemethanol compounds have been found 30 years ago to show anti-malarial effects in the avian malaria model. Among them, SN10,275 has long-lasting hemophilic schizonts on human Plasmodium vivax, but can not be widely used due to phototoxicity. WR30,090 is sensitive to chloroquine sensitive strains or resistant strains of Plasmodium falciparum, and has the least phototoxicity. However, the time for killing schistosomes is quite short. Mefloquine demonstrated by preclinical studies was better than WR30,090