STRUCTURE-ACTIVITY-RELATIONSHIPS OF SOME GALBULIMIMA ALKALOIDS RELATED TO HIMBACINE

被引：30

作者：

DARROCH, SA

TAYLOR, WC

CHOO, LK

MITCHELSON, F

机构：

[1] VICTORIAN COLL PHARM,SCH PHARMACOL,381 ROYAL PARADE,PARKVILLE,VIC 3052,AUSTRALIA

[2] UNIV SYDNEY,DEPT ORGAN CHEM,SYDNEY,NSW 2006,AUSTRALIA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 182卷 / 01期

基金：

英国医学研究理事会;

关键词：

Himbacine; Muscarinic receptor antagonists (cardioselective);

D O I：

10.1016/0014-2999(90)90501-V

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Himbacine, himbeline, N-methylhimandravine and himandravine together with their dihydro-derivatives were evaluated as antagonists of muscarinic receptors in guinea-pig ileal longitudinal muscle and electrically stimulated left atrium. Himbacine was the most potent compound and the 15-fold selectivity exhibited for the M2 muscarinic receptor was greater than that found with any of the other compounds examined. Reduction of the double bond linking the decalin ring system and the piperidine ring almost abolished selectivity in dihydrohimbacine. Removal of the N-methyl group in himbacine to form himbeline with reduced selectivity. However the corresponding change in converting N-methylhimandravine to himandravine was not associated with any change in selectivity suggesting that orientation of the 2-methyl group in the piperidine ring may be important for selectivity. © 1990.

引用

页码：131 / 136

页数：6

共 15 条

[1] SOME QUANTITATIVE USES OF DRUG ANTAGONISTS [J].