氯喹对映体和去乙基氯喹的蛋白结合
Protein binding of chloroquine enantiomers and desethylchloroquine.
作者信息
Ofori-Adjei D, Ericsson O, Lindström B, Sjöqvist F
出版信息
Br J Clin Pharmacol. 1986 Sep;22(3):356-8. doi: 10.1111/j.1365-2125.1986.tb02900.x.
Abstract
The protein binding of racemic chloroquine, its enantiomers and desethylchloroquine to plasma, purified human albumin, and alpha 1-acid glycoprotein (alpha 1-AGP) was determined by equilibrium dialysis. The binding was not concentration dependent. (+)-Chloroquine bound more to plasma (66.6 +/- 1.9%) and albumin (45.9 +/- 0.8%) than (-)-chloroquine (48.5 +/- 2.4% and 35.3 +/- 0.6%, respectively). These differences were statistically significant. (-)-Chloroquine bound more to alpha 1-AGP (47.5 +/- 0.7%) than (+)-chloroquine (34.5 +/- 0.5%). The binding of desethylchloroquine to alpha 1-AGP is higher than to albumin (38.9 +/- 0.9% and 21.1 +/- 0.4%, respectively.
摘要
通过平衡透析法测定了消旋氯喹、其对映体和去乙基氯喹与血浆、纯化的人白蛋白及α1-酸性糖蛋白（α1-AGP）的蛋白结合情况。这种结合不依赖于浓度。（+）-氯喹与血浆（66.6±1.9%）和白蛋白（45.9±0.8%）的结合比（-）-氯喹（分别为48.5±2.4%和35.3±0.6%）更多。这些差异具有统计学意义。（-）-氯喹与α1-AGP（47.5±0.7%）的结合比（+）-氯喹（34.5±0.5%）更多。去乙基氯喹与α1-AGP的结合高于与白蛋白的结合（分别为38.9±0.9%和21.1±0.4%）。
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