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加拉明和泮库溴铵可抑制犬隐静脉中节前和节后毒蕈碱受体。

Gallamine and pancuronium inhibit pre- and postjunctional muscarine receptors in canine saphenous veins.

作者信息

Vercruysse P, Bossuyt P, Hanegreefs G, Verbeuren T J, Vanhoutte P M

出版信息

J Pharmacol Exp Ther. 1979 May;209(2):225-30.

PMID:438998
Abstract

The influence of gallamine, pancuronium, suxamethonium and d-tubocurarine on adrenergic neurotransmission was studied in the isolated saphenous vein of the dog. Pancuronium but not the other muscle relaxants increased significantly the response to sympathetic stimulation and to exogenous norepipephrine; these increases were abolished after blockade of neuronal uptake by cocaine. Pancuronium and gallamine inhibited both the relaxation produced by lower doses of acetylcholine added during sympathetic stimulation (prejunctional effect) and the direct contractions evoked by high doses of the amine (postjunctional effect). In strips previously incubated with [3H]norepinephrine, gallamine had no effect on [3H]norepinephrine efflux in basal conditions and during sympathetic stimulation; it increased markedly the efflux evoked by sympathetic stimulation in the presence of acetylcholine confirming that gallamine inhibits the prejunctional effect of the latter on adrenergic transmission. When extrapolated to the intact organism, the present experiments indicate that gallamine and pancuronium augment the release of norepinephrine in vascular tissue under vagal control, which explains in part the cardiovascular effects of these muscle relaxants.

摘要

在犬离体隐静脉中研究了加拉明、泮库溴铵、琥珀酰胆碱和d -筒箭毒碱对肾上腺素能神经传递的影响。泮库溴铵能显著增强对交感神经刺激和外源性去甲肾上腺素的反应,而其他肌肉松弛剂则无此作用;在用可卡因阻断神经元摄取后,这些增强作用消失。泮库溴铵和加拉明既能抑制交感神经刺激期间添加的较低剂量乙酰胆碱所产生的舒张作用(接头前效应),又能抑制高剂量胺所诱发的直接收缩作用(接头后效应)。在预先用[³H]去甲肾上腺素孵育过的组织条中,加拉明在基础状态和交感神经刺激期间对[³H]去甲肾上腺素的外流均无影响;在乙酰胆碱存在的情况下,它能显著增加交感神经刺激所诱发的外流,证实加拉明抑制了乙酰胆碱对肾上腺素能传递的接头前效应。当外推至完整机体时,本实验表明加拉明和泮库溴铵可增强迷走神经控制下血管组织中去甲肾上腺素的释放,这部分解释了这些肌肉松弛剂的心血管效应。

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