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洛贝林对神经元型和肌肉型烟碱受体的不同作用。

Different effects of lobeline on neuronal and muscle nicotinic receptors.

作者信息

Kaniakova Martina, Skrenkova Kristyna, Adamek Svatopluk, Vyskocil Frantisek, Krusek Jan

机构信息

Institute of Physiology, Academy of Sciences of the Czech Republic, v.v.i., Vídeňská 1083, 142 20 Prague 4, Czech Republic.

Institute of Physiology, Academy of Sciences of the Czech Republic, v.v.i., Vídeňská 1083, 142 20 Prague 4, Czech Republic; Department of Physiology, Faculty of Science, Charles University, Viničná 7, 120 00 Prague, Czech Republic.

出版信息

Eur J Pharmacol. 2014 Sep 5;738:352-9. doi: 10.1016/j.ejphar.2014.05.057. Epub 2014 Jun 12.

Abstract

Lobeline is a plant alkaloid known to interact with cholinergic system. The effect of lobeline on neuronal α3β4 receptors expressed in COS cells and muscle embryonic αβγδ receptors naturally expressed in TE671 cells was studied using a patch-clamp technique. Our results show that lobeline inhibited responses to acetylcholine in human embryonic muscle nicotinic receptor in a pseudo-noncompetitive manner. The responses of rat neuronal α3β4 receptors to a low concentration of acetylcholine were potentiated by a mixed occupation mechanism that corresponds to "competitive potentiation". This potentiation turned into voltage-dependent inhibition for α3β4 receptors was activated by a high concentration of acetylcholine.

摘要

洛贝林是一种已知可与胆碱能系统相互作用的植物生物碱。采用膜片钳技术研究了洛贝林对COS细胞中表达的神经元α3β4受体以及TE671细胞中天然表达的肌肉胚胎αβγδ受体的作用。我们的结果表明,洛贝林以伪非竞争性方式抑制人胚胎肌肉烟碱样受体对乙酰胆碱的反应。大鼠神经元α3β4受体对低浓度乙酰胆碱的反应通过一种对应于“竞争性增强”的混合占据机制得到增强。当α3β4受体被高浓度乙酰胆碱激活时,这种增强转变为电压依赖性抑制。

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