Muscarinic receptor agonists and antagonists: effects on cardiovascular function.
Muscarinic receptor agonists and antagonists: effects on cardiovascular function.
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DOI：
10.1007/978-3-642-23274-9_13
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发表时间：
2012-01-01
影响因子：
--
通讯作者：
Harvey, Robert D
中科院分区：
文献类型：
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作者：
Harvey, Robert D
毒蕈碱受体激活在心血管功能的副交感神经调节中起着重要作用。副交感神经刺激的主要作用是通过抑制心率来减少心输出量。然而，从药理学上来说，毒蕈碱激动剂实际上能够对心脏和脉管系统产生抑制和刺激作用。这反映了毒蕈碱受体在整个心血管系统中表达的事实，尽管它们并不总是参与介导副交感神经反应。在心脏中，除了通过改变窦房结的电活动来调节心率之外，M2受体的激活还可以影响通过房室结的电脉冲的传导。这些相同的受体还可以调节心房和心室的电和机械活动。在脉管系统中，上皮细胞中M₃和M₅受体的激活可引起血管舒张，而血管平滑肌细胞中M₁或M₃受体的激活可在没有内皮的情况下引起血管收缩。本综述重点关注我们目前对介导这些反应的信号机制的理解。
Muscarinic receptor activation plays an essential role in parasympathetic regulation of cardiovascular function. The primary effect of parasympathetic stimulation is to decrease cardiac output by inhibiting heart rate. However, pharmacologically, muscarinic agonists are actually capable of producing both inhibitory and stimulatory effects on the heart as well as vasculature. This reflects the fact that muscarinic receptors are expressed throughout the cardiovascular system, even though they are not always involved in mediating parasympathetic responses. In the heart, in addition to regulating heart rate by altering the electrical activity of the sinoatrial node, activation of M₂ receptors can affect conduction of electrical impulses through the atrioventricular node. These same receptors can also regulate the electrical and mechanical activity of the atria and ventricles. In the vasculature, activation of M₃ and M₅ receptors in epithelial cells can cause vasorelaxation, while activation of M₁ or M₃ receptors in vascular smooth muscle cells can cause vasoconstriction in the absence of endothelium. This review focuses on our current understanding of the signaling mechanisms involved in mediating these responses.