PHARMACOLOGICAL PROPERTIES OF THE HOMOMERIC ALPHA-7 RECEPTOR

被引:110
作者
BERTRAND, D [1 ]
BERTRAND, S [1 ]
BALLIVET, M [1 ]
机构
[1] DEPT BIOCHEM,GENEVA,SWITZERLAND
关键词
NEURONAL; NICOTINIC ACETYLCHOLINE RECEPTOR; ALPHA-BUNGAROTOXIN; PHARMACOLOGY; ELECTROPHYSIOLOGY; XENOPUS OOCYTE;
D O I
10.1016/0304-3940(92)90179-B
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
The pharmacological properties of the alpha-bungarotoxin sensitive alpha7 neuronal nicotinic acetylcholine receptor (nAChR) were studied upon reconstitution in Xenopus oocytes. Channels formed by alpha7 are about 10-fold more sensitive to nicotine and cytisine than to ACh but are little, if at all, activated by the ganglionic agonist 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP). Tubocurarine (TC) was found to act as a non-competitive inhibitor, whereas dihydro-beta-erythroidine (DHbetaE) behaves as a pure competitive inhibitor whose blockade is fast and fully reversible. In addition, the alpha7 receptor displays a poor sensitivity to methonium salts. The pharmacological properties of the alpha7 channels are readily distinguishable from those of other identified neuronal nicotinic receptors.
引用
收藏
页码:87 / 90
页数:4
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