AGONIST PHARMACOLOGY OF THE NEURONAL ALPHA-7 NICOTINIC RECEPTOR EXPRESSED IN XENOPUS-OOCYTES

被引：61

作者：

AMAR, M ^{[1
]}

THOMAS, P ^{[1
]}

JOHNSON, C ^{[1
]}

LUNT, GG ^{[1
]}

WONNACOTT, S ^{[1
]}

机构：

[1] UNIV BATH,DEPT BIOCHEM,BATH BA2 7AY,AVON,ENGLAND

来源：

FEBS LETTERS | 1993年 / 327卷 / 03期

关键词：

NEURONAL NICOTINIC RECEPTOR; NICOTINIC AGONIST; (+)-ANATOXIN-A; NICOTINE; ALPHA-BUNGAROTOXIN; XENOPUS OOCYTE;

D O I：

10.1016/0014-5793(93)81005-K

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The potencies and efficacies of seven agonists at chick alpha7 nicotinic receptors expressed in Xenopus oocytes were determined by whole cell recording. (+)-Anatoxin-a was the most potent agonist (EC50 = 0.58 muM) and acetylcholine was the least potent (EC50 = 320 muM). The rank order of agonist potencies was: (+)-anatoxin-a >> cytisine > (-)-nicotine > (+)-nicotine > DMPP > 1-acetyl-4-methylpiperazine methiodide > acetylcholine. DMPP evoked only very small currents: comparison of maximally effective agonist concentrations showed that DMPP was only one-fifth as efficacious as other agonists. Previously published IC50 values for rat brain [I-125]alpha-bungarotoxin sites show a similar agonist profile, and the identity of homo-oligomeric alpha7 receptors with native alpha-bungarotoxin-sensitive neuronal nicotinic receptors is discussed.

引用

页码：284 / 288

页数：5

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