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阿司匹林对脑内5-羟色胺和甲硫氨酸脑啡肽的影响:与药物的抗伤害感受活性的相关性。

Effect of aspirin on serotonin and met-enkephalin in brain: correlation with the antinociceptive activity of the drug.

作者信息

Groppetti A, Braga P C, Biella G, Parenti M, Rusconi L, Mantegazza P

机构信息

Department of Pharmacology Emilio Trabucchi, University of Milan, Italy.

出版信息

Neuropharmacology. 1988 May;27(5):499-505. doi: 10.1016/0028-3908(88)90132-3.

Abstract

Intravenous administration of acetyl salicylate of lysine, a soluble salt of aspirin, reduced in rats the firing discharge of thalamic neurones, evoked by noxious stimuli. Concomitantly, concentrations of 5-hydroxyindole acetic acid increased, while those of met-enkephalin-like immuno-reactive derivatives were decreased in several areas of the brain. Similar electrophysiological and biochemical responses were obtained by administering tryptophan or 5-hydroxytryptophan plus carbidopa. The effect of aspirin on the evoked firing of the thalamic neurones was counteracted by pretreating the animals with metergoline. On the other hand, naloxone did not antagonize the inhibitory effect of aspirin and 5-hydroxytryptophan on pain-induced neuronal excitation. These data indicate that a serotonin-, but not a naloxone-sensitive opiate mechanism, may be relevant for aspirin-mediated antinociception.

摘要

静脉注射赖氨酸乙酰水杨酸(阿司匹林的一种可溶性盐)可减少大鼠丘脑神经元由有害刺激诱发的放电。与此同时,大脑多个区域的5-羟吲哚乙酸浓度升高,而甲硫氨酸脑啡肽样免疫反应性衍生物的浓度降低。通过给予色氨酸或5-羟色氨酸加卡比多巴也可获得类似的电生理和生化反应。用美替拉酮预处理动物可抵消阿司匹林对丘脑神经元诱发放电的影响。另一方面,纳洛酮不能拮抗阿司匹林和5-羟色氨酸对疼痛诱导的神经元兴奋的抑制作用。这些数据表明,5-羟色胺介导而非纳洛酮敏感的阿片类机制可能与阿司匹林介导的镇痛作用有关。

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