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ω-芋螺毒素GVIA通过阻断牛嗜铬细胞中烟碱受体激活的内向电流,来阻断尼古丁诱导的儿茶酚胺分泌。

omega-Conotoxin GVIA blocks nicotine-induced catecholamine secretion by blocking the nicotinic receptor-activated inward currents in bovine chromaffin cells.

作者信息

Fernández J M, Granja R, Izaguirre V, González-García C, Ceña V

机构信息

Departamento de Farmacología, Universidad de Alicante, Spain.

出版信息

Neurosci Lett. 1995 May 19;191(1-2):59-62. doi: 10.1016/0304-3940(95)11558-x.

Abstract

We have studied the contribution of N-type voltage-dependent Ca2+ channels to both norepinephrine and epinephrine secretion from bovine chromaffin cells induced by high K+ or nicotine using omega-conotoxin GVIA, a selective blocker of N-type voltage-dependent Ca2+ channels. We found that high K+ (75 mM) induced catecholamine secretion was not affected by exposure of bovine chromaffin cells to omega-conotoxin GVIA (1 microM). However, nicotine-induced both norepinephrine and epinephrine secretion were similarly blocked (about 25%) by omega-conotoxin GVIA (1 microM). This effect could be explained by a potent (about 80%) and reversible blockade of the inward current induced by nicotine receptor activation in bovine chromaffin cells. The results indicate that besides the blockade of N-type voltage-dependent channels, omega-conotoxin GVIA is a potent and reversible blocker of the nicotinic receptor-induced currents in chromaffin cells.

摘要

我们使用N型电压依赖性Ca2+通道的选择性阻滞剂ω-芋螺毒素GVIA,研究了N型电压依赖性Ca2+通道对高钾或尼古丁诱导的牛嗜铬细胞去甲肾上腺素和肾上腺素分泌的作用。我们发现,高钾(75 mM)诱导的儿茶酚胺分泌不受牛嗜铬细胞暴露于ω-芋螺毒素GVIA(1 μM)的影响。然而,ω-芋螺毒素GVIA(1 μM)同样阻断了尼古丁诱导的去甲肾上腺素和肾上腺素分泌(约25%)。这种效应可以通过牛嗜铬细胞中尼古丁受体激活诱导的内向电流的有效(约80%)和可逆阻断来解释。结果表明,除了阻断N型电压依赖性通道外,ω-芋螺毒素GVIA还是嗜铬细胞中烟碱受体诱导电流的有效和可逆阻滞剂。

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