PHARMACOLOGICAL PROPERTIES OF THE HOMOMERIC ALPHA-7 RECEPTOR
PHARMACOLOGICAL PROPERTIES OF THE HOMOMERIC ALPHA-7 RECEPTOR
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DOI：
10.1016/0304-3940(92)90179-b
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发表时间：
1992-10-26
影响因子：
2.5
通讯作者：
BALLIVET, M
中科院分区：
文献类型：
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作者：
BERTRAND, D;BERTRAND, S;BALLIVET, M
研究了α-银环蛇毒素敏感的α-7神经元烟碱型乙酰胆碱受体(NAChR)在非洲爪哇卵母细胞重组时的药理学特性。Alpha7形成的通道对尼古丁和胱氨酸的敏感性约为ACh的10倍，但几乎不被神经节激动剂1，1-二甲基-4-苯基哌嗪碘(DMPP)激活。Tubocurarine(TC)是一种非竞争性的抑制剂，而二氢-β-乙酸乙二胺(DHbetaE)是一种纯竞争性的抑制剂，其阻断是快速且完全可逆的。此外，Alpha7受体对甲烷盐的敏感性较差。α7通道的药理学特性很容易与其他已发现的神经性尼古丁受体区别开来。
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.