Webster R V, Craig J C, Shyamala V, Kirby G C, Warhurst D C
Department of Pharmaceutical Chemistry, University of California, San Francisco 94143-0446.
Biochem Pharmacol. 1991 Dec 11;42 Suppl:S225-7. doi: 10.1016/0006-2952(91)90417-4.
Both enantiomers of quinacrine and the racemic form of the drug showed equal activity in vitro against chloroquine-sensitive and -resistant strains of Plasmodium falciparum, without detectable stereoselectivity. This contrasts with observations on chloroquine, where a similar lack of stereoselectivity in vitro is accompanied by a 10-fold loss of activity against the resistant strain. The observed in vivo differences reported for the enantiomers of chloroquine and the observations on the optically active metabolites of chloroquine and quinacrine may therefore be ascribed to a difference in the pharmacokinetics of their enantiomers.
喹吖因的两种对映体以及该药物的外消旋形式在体外对氯喹敏感和耐药的恶性疟原虫菌株均表现出同等活性，无明显的立体选择性。这与氯喹的情况形成对比，氯喹在体外同样缺乏立体选择性，但对耐药菌株的活性却损失了10倍。因此，所报道的氯喹对映体在体内的差异以及对氯喹和喹吖因光学活性代谢物的观察结果，可能归因于它们对映体在药代动力学上的差异。
