BINDING OF TROPANE ALKALOIDS TO NICOTINIC AND MUSCARINIC ACETYLCHOLINE RECEPTORS

被引：0
|
作者：
SCHMELLER, T [1 ]
SPORER, F [1 ]
SAUERWEIN, M [1 ]
WINK, M [1 ]
机构：
[1] UNIV HEIDELBERG,INST PHARMAZEUT BIOL,D-69120 HEIDELBERG,GERMANY
来源：
PHARMAZIE | 1995年 / 50卷 / 07期
关键词：
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Fourteen tropane and related alkaloids were analyzed for their affinity for nicotinic and/or muscarinic acetylcholine receptors. The biogenetic intermediates littorine, 6 beta-hydroxyhyoscyamine, 7 beta-hydroxyhyoscyamine exhibit similar affinities at the muscarinic receptor as scopolamine and atropine. The quarternary derivatives N-methylatropine and N-methylscopolamine show the highest binding with IC50 values of less than 100 pM and 300 pM, respectively. The tropane alkaloids (including cocaine) also bind to the nicotinic acetylcholine receptor, albeit with much lower affinities.
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页码：493 / 495
页数：3
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