PREGNANE AND 21-NORPREGNANE DERIVATIVES OF OUABAIN THAT BIND TO THE DIGITALIS RECEPTOR

被引:4
作者
TEMPLETON, JF
LING, Y
ZEGLAM, TH
MARAT, K
LABELLA, FS
机构
[1] UNIV MANITOBA,DEPT CHEM,WINNIPEG R3T 2N2,MB,CANADA
[2] UNIV MANITOBA,DEPT PHARMACOL & THERAPEUT,WINNIPEG R3E 0W3,MB,CANADA
基金
英国医学研究理事会;
关键词
14-BETA-HYDROXYPREGNANE GLYCOSIDE; 14-BETA-HYDROXY-21-NORPREGNANE GLYCOSIDE; OUABAIN; CARDIAC GLYCOSIDE RECEPTOR BINDING; RADIOLIGAND BINDING ASSAY;
D O I
10.1016/0223-5234(94)90140-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
14 beta-Hydroxy-5 beta-pregnane and 14 beta-hydroxy-21-nor-5 beta-pregnane derivatives of ouabain were synthesised and their structures established by NMR measurements. Binding affinity in an [H-3]ouabain radioligand binding assay was determined. Pregnane derivatives of ouabain are more polar than pregnane rhamnoside derivatives of digitoxigenin. Whereas ouabain binds similarly to digitoxigenin rhamnoside, the pregnane derivatives of ouabain have significantly weaker binding affinity than their congeners from digitoxigenin.
引用
收藏
页码:799 / 804
页数:6
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