Braga P C, Biella G, Tiengo M, Fraschini F
Neuropharmacology. 1986 Sep;25(9):1055-62. doi: 10.1016/0028-3908(86)90202-9.
The effects of suprofen, a new non-steroidal anti-inflammatory drug, (NSAID), the activity of which is mainly antinociceptive, were compared with those of aspirin (as a reference drug) in a study of spontaneous and evoked firing of thalamic neurons (nucleus lateralis and ventrobasalis) in rats rendered arthritic by injection of Freund's adjuvant into the paw. Suprofen (3.7 mg/kg, i.v.) induced a marked decrease in the firing evoked in arthritic rats by ankle mobilization. This effect, after a rapid onset, lasted on the average for 60 min. A similar effect was obtained with aspirin, but with 54 mg/kg (i.v.) (14 times more than suprofen). With increasing doses of suprofen, it was possible to obtain an increased long-lasting inhibition of the evoked activity, with a significant dose-effect linear regression. The possibility that there are both CNS and peripheral effects of suprofen is discussed in relation to the possible role of aspirin (the reference standard for NSAIDs) in enhancing presynaptic inhibition, thus reducing the effectiveness of incoming sensory stimuli.
在一项对通过向大鼠爪子注射弗氏佐剂而诱发关节炎的实验中,研究了新型非甾体抗炎药(NSAID)舒洛芬(其活性主要为抗伤害感受)与阿司匹林(作为参比药物)对丘脑神经元(外侧核和腹基底核)自发放电和诱发放电的影响。舒洛芬(3.7毫克/千克,静脉注射)可使关节炎大鼠踝关节活动诱发的放电显著减少。该效应起效迅速,平均持续60分钟。阿司匹林(54毫克/千克,静脉注射)(是舒洛芬的14倍)也可产生类似效应。随着舒洛芬剂量增加,可实现对诱发放电的增强且持久的抑制,呈现显著的剂量效应线性回归。结合阿司匹林(NSAIDs的参比标准)在增强突触前抑制从而降低传入感觉刺激有效性方面的可能作用,讨论了舒洛芬存在中枢神经系统和外周效应的可能性。