Otton S V, Kalow W, Seeman P
Experientia. 1984 Sep 15;40(9):973-4. doi: 10.1007/BF01946465.
The techniques of the radioreceptor binding assay were applied to detect stereoselective binding of quinidine and quinine to a site on human liver microsomes. Binding of 3H-dihydroquinidine was 50% inhibited by 20-100 nM quinidine, while its enantiomer quinine did not displace the 3H-ligand at concentrations up to 500 nM. This stereoselectivity agreed with the affinity values measured by functional enzyme assays of cytochrome P450 activity using sparteine or debrisoquine as substrates.
采用放射受体结合分析技术检测奎尼丁和奎宁与人肝微粒体上某一位点的立体选择性结合。20 - 100 nM的奎尼丁可抑制3H - 二氢奎尼丁50%的结合，而其对映体奎宁在浓度高达500 nM时不能取代3H配体。这种立体选择性与使用司巴丁或异喹胍作为底物通过细胞色素P450活性功能酶分析测得的亲和力值一致。
