Muscarinic cationic current in gastrointestinal smooth muscles: signal transduction and role in contraction

Muscarinic cationic current in gastrointestinal smooth muscles: signal transduction and role in contraction
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DOI:
10.1111/j.1474-8673.2006.00366.x
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发表时间:
2006-07-01
期刊:
Autonomic & Autacoid Pharmacology
影响因子:
--
通讯作者:
Komori, S.
Komori, S.
中科院分区:
其他
文献类型:
--
作者:
Unno, T.;Matsuyama, H.;Komori, S.

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1毒蕈碱受体在包括胃肠道在内的各种外周组织的副交感神经控制中起关键作用。神经递质乙酰胆碱通过激活存在于平滑肌中的毒蕈碱受体产生收缩。2阳离子通道的开放是一种潜在机制。阳离子通道的开放导致Ca2+通过通道流入细胞,也通过电压依赖性Ca2+通道,其响应于去极化而二次打开,提供一定量的Ca2+用于激活收缩蛋白。3电生理学和药理学研究表明,阳离子通道以及毒蕈碱受体存在于许多内脏平滑肌细胞中。然而,阳离子通道的激活机制仍然不清楚。4在这篇文章中,我们总结了毒蕈碱受体操纵的阳离子通道的现有知识,重点是受体亚型,G蛋白和其他信号分子参与这些通道的激活和通道的分子特征。这将改善旨在开发新的选择性药理学试剂和理解这些通道在生理系统中的激活机制和功能的策略。
1 The muscarinic receptor plays a key role in the parasympathetic nervous control of various peripheral tissues including gastrointestinal tract. The neurotransmitter acetylcholine, via activating muscarinic receptors that exist in smooth muscle, produces its contraction.2 There is the opening of cationic channels as an underlying mechanism. The opening of cationic channels results in influxes of Ca2+ via the channels into the cell and also via voltage-dependent Ca2+ channels which secondarily opened in response to the depolarization, providing an amount of Ca2+ for activation of the contractile proteins.3 Electrophysiological and pharmacological studies have shown that the cationic channels as well as muscarinic receptors exist in many visceral smooth muscle cells. However, the activation mechanisms of the cationic channels are still unclear.4 In this article, we summarize the current knowledge of the muscarinic receptor-operated cationic channels, focusing on the receptor subtype, G protein and other signalling molecules that are involved in activation of these channels and on the molecular characterisitics of the channel. This will improve strategies aimed at developing new selective pharmacological agents and understanding the activation mechanism and functions of these channels in physiological systems.