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酮洛芬:脑室内注射与抗伤害感受作用的电生理方面

Ketoprofen: i.c.v. injection and electrophysiological aspects of antinociceptive effect.

作者信息

Braga P C

机构信息

Department of Pharmacology, Chemotherapy and Toxicology, School of Medicine, University of Milan, Italy.

出版信息

Eur J Pharmacol. 1990 Aug 10;184(2-3):273-80. doi: 10.1016/0014-2999(90)90619-h.

DOI:10.1016/0014-2999(90)90619-h
PMID:2079099
Abstract

The direct action of ketoprofen on the CNS was investigated by electrophysiological techniques in rats made arthritic. Between the 10th and 16th days after the administration of the complete Freund's adjuvant the rats were anesthetized and the drug was injected directly into the cerebral ventricles. The changes in spontaneous and evoked firing of thalamic neurons were investigated. Ketroprofen very rapidly inhibited the nociceptive activity induced by ankle mobilization. The inhibitory effects were maximal at the doses of 20 and 40 micrograms within 5 min and spontaneous activity was also reduced. The time courses of the action of the increasing doses were also measured. In view of the site of injection, the doses and the very rapid start of the effects, the inhibition of spontaneous and evoked neuronal firing supports the view of a direct effect of this drug on the electrical behaviour of the neurons.

摘要

通过电生理技术,在患有关节炎的大鼠身上研究了酮洛芬对中枢神经系统的直接作用。在注射完全弗氏佐剂后的第10天至第16天之间,将大鼠麻醉,然后将药物直接注入脑室。研究了丘脑神经元自发放电和诱发放电的变化。酮洛芬能非常迅速地抑制踝关节活动诱导的伤害性活动。在5分钟内,20微克和40微克剂量的抑制作用最大,自发放电也减少。还测量了递增剂量作用的时间进程。鉴于注射部位、剂量以及作用起效非常迅速,自发和诱发性神经元放电的抑制支持了该药物对神经元电活动有直接作用的观点。

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