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毒蕈碱受体 - G蛋白偶联的破坏是液体挥发性麻醉剂的普遍特性。

Disruption of muscarinic receptor-G protein coupling is a general property of liquid volatile anesthetics.

作者信息

Anthony B L, Dennison R L, Aronstam R S

机构信息

Department of Pharmacology and Toxicology, Medical College of Georgia, Augusta 30912.

出版信息

Neurosci Lett. 1989 Apr 24;99(1-2):191-6. doi: 10.1016/0304-3940(89)90288-7.

Abstract

The influences of 3 volatile anesthetics, chloroform, enflurane and isoflurane, on muscarinic acetylcholine receptors in rat brainstem were determined. Each of the volatile anesthetics increased [3H]methylscopolamine [( 3H]MS) binding affinity, but did not affect the number of [3H]MS binding sites. Carbamylcholine affinity for brainstem muscarinic receptors was not altered after equilibration of brainstem membranes with any of these anesthetics. The ability of guanine nucleotides to depress the high affinity binding of two agonists, carbamylcholine and [3H]oxotremorine-M, was decreased or eliminated after equilibration of brainstem membranes with any of the anesthetics. In each of these actions, these anesthetics resemble halothane and diethyl ether. These results indicate that interference with muscarinic receptor-G protein interactions is a common property of liquid volatile anesthetics and may represent a general mechanism for the disruption of signal transmission between cells during anesthesia.

摘要

测定了三种挥发性麻醉剂氯仿、安氟醚和异氟醚对大鼠脑干毒蕈碱型乙酰胆碱受体的影响。每种挥发性麻醉剂均增加了[³H]甲基东莨菪碱([³H]MS)的结合亲和力,但不影响[³H]MS结合位点的数量。在用这些麻醉剂中的任何一种平衡脑干膜后,氨甲酰胆碱对脑干毒蕈碱受体的亲和力未发生改变。在用这些麻醉剂中的任何一种平衡脑干膜后,鸟嘌呤核苷酸抑制两种激动剂氨甲酰胆碱和[³H]氧震颤素-M高亲和力结合的能力降低或消除。在这些作用中,这些麻醉剂类似于氟烷和乙醚。这些结果表明,干扰毒蕈碱受体-G蛋白相互作用是液体挥发性麻醉剂的共同特性,可能代表麻醉期间细胞间信号传递中断的一般机制。

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