Fitch C D
Antimicrob Agents Chemother. 1973 May;3(5):545-8. doi: 10.1128/AAC.3.5.545.
(14)C-amodiaquin and (14)C-chloroquine were used to study drug binding by preparations of owl monkey erythrocytes infected either with a chloroquine-susceptible (CS) or with a chloroquine-resistant (CR) strain of P. falciparum. Both of these drugs are derivatives of 4-aminoquinoline, but they differ in their side chains, and there are differences in the way they are handled by preparations of erythrocytes infected with malaria parasites. Although the apparent association constant for the binding of either drug is approximately 10(7) mol(-1), two to three times more radioactivity was bound from (14)C-amodiaquin than from (14)C-chloroquine. Furthermore, there was no apparent difference between CS and CR parasites with respect to (14)C-amodiaquin binding, whereas erythrocytes infected with CR parasites have a deficiency of (14)C-chloroquine binding. This difference in the handling of amodiaquin probably accounts for its superiority in the treatment of the owl monkey and of humans infected with CR P. falciparum.
使用（14）C-阿莫地喹和（14）C-氯喹来研究感染对氯喹敏感（CS）或耐氯喹（CR）恶性疟原虫株的夜猴红细胞制剂的药物结合情况。这两种药物都是4-氨基喹啉的衍生物，但它们的侧链不同，并且感染疟原虫的红细胞制剂对它们的处理方式也存在差异。尽管两种药物结合的表观缔合常数约为10（7）mol（-1），但从（14）C-阿莫地喹结合的放射性比从（14）C-氯喹结合的多两到三倍。此外，就（14）C-阿莫地喹结合而言，CS和CR寄生虫之间没有明显差异，而感染CR寄生虫的红细胞对（14）C-氯喹的结合存在缺陷。阿莫地喹处理方式的这种差异可能解释了其在治疗感染CR恶性疟原虫的夜猴和人类方面的优越性。
