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G蛋白偶联受体

G-protein-coupled receptors.

作者信息

Sanders R D, Brian D, Maze M

机构信息

Academic Anaesthetics, Imperial College, Chelsea & Westminster Hospital, 369 Fulham Road, London, SW10 9NH, UK,

出版信息

Handb Exp Pharmacol. 2008(182):93-117. doi: 10.1007/978-3-540-74806-9_5.

Abstract

G-Protein-coupled receptors mediate many of the hypnotic and analgesic actions of the drugs employed in anesthesia. Notably, opioid agonists represent the most successful and efficacious class of analgesic agents employed over the last century. Also, major clinical advances have been made by the study of alpha(2) adrenoceptor agonists, which possess both hypnotic and analgesic qualities that are being increasingly exploited in both anesthetic and critical care settings. Furthermore orexin, gamma-aminobutyric acid (GABA) (B), and muscarinic cholinergic receptors have been identified as potential anesthetic targets; clinical exploitation of ligands at these receptors may lead to important advances in anesthetic pharmacology. In this review we discuss the relevant molecular and neural network pharmacology of anesthetic agents acting at G-protein-coupled receptors.

摘要

G蛋白偶联受体介导了麻醉用药的许多催眠和镇痛作用。值得注意的是,阿片类激动剂是上个世纪使用的最成功、最有效的一类镇痛药物。此外,对α₂肾上腺素能受体激动剂的研究取得了重大临床进展,这类药物兼具催眠和镇痛特性,在麻醉和重症监护环境中得到了越来越多的应用。此外,食欲素、γ-氨基丁酸(GABA)(B)和毒蕈碱胆碱能受体已被确定为潜在的麻醉靶点;作用于这些受体的配体的临床应用可能会在麻醉药理学方面带来重要进展。在这篇综述中,我们讨论了作用于G蛋白偶联受体的麻醉药物的相关分子和神经网络药理学。

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