DELPHINIUM ALKALOIDS AS INHIBITORS OF ALPHA-BUNGAROTOXIN BINDING TO RAT AND INSECT NEURAL MEMBRANES

被引：49

作者：

KUKEL, CF

JENNINGS, KR

机构：

[1] YORK UNIV,DEPT BIOL,4700 KEELE ST,N YORK M3J 1A1,ON,CANADA

[2] CYANAMID CANADA INC,MARKHAM L3R 6E6,ON,CANADA

来源：

CANADIAN JOURNAL OF PHYSIOLOGY AND PHARMACOLOGY | 1994年 / 72卷 / 01期

关键词：

NICOTINIC; ACETYLCHOLINE; DELPHINIUM; DITERPENOID;

D O I：

10.1139/y94-016

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A series of C19-diterpenoid alkaloids purified from Delphinium were evaluated as inhibitors of alpha-bungarotoxin binding to rat and house fly neural membranes. In comparing these diterpenoid analogs, a wide range of inhibition potencies (IC50) were observed, with calculated IC50 values ranging six orders of magnitude. The most potent inhibitory alkaloids in this series possessed the succinimide aromatic ester moiety in the C18 position. Glaudelsine had an IC50 value of 42 pM at the insect nicotinic acetylcholine receptor.

引用

页码：104 / 107

页数：4

共 14 条

[1] PRINCIPAL TOXIN OF DELPHINIUM-BROWNII RYDB, AND ITS MODE OF ACTION [J].