ANTINOCICEPTIVE EFFECTS OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS IN A RAT MODEL OF UNILATERAL HINDPAW INFLAMMATION
ANTINOCICEPTIVE EFFECTS OF NONSTEROIDAL ANTIINFLAMMATORY DRUGS IN A RAT MODEL OF UNILATERAL HINDPAW INFLAMMATION
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DOI：
10.1016/0014-2999(94)90700-5
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发表时间：
1994-05-12
影响因子：
5
通讯作者：
SPANGLER, RS
中科院分区：
文献类型：
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作者：
CLARKE, GD;MACPHERSON, IS;SPANGLER, RS
在大鼠单侧后爪炎症/痛觉过敏模型中检测了肌肉注射萘丁美酮的活性代谢产物6-甲氧基-2-萘乙酸（6-MNA）的镇痛活性，并与其他三种非甾体抗炎药（NSAIDs）-双氯芬酸、萘丁美酮和吡罗昔康的镇痛活性进行了比较。在10-100 mg/kg i.m.的剂量范围内，6-MNA产生了剂量依赖性的增加，在撤回阈值的有害机械刺激施加到发炎的爪子;然而，更高的剂量（300毫克/公斤）产生的抗伤害活性没有进一步增加。肌内注射后30 min出现峰值效应。双氯芬酸、萘普生和吡罗昔康产生的镇痛作用在性质上与6-MNA相似。四种NSAID之间在效价和疗效方面存在定量差异，但无统计学显著性。快速起效和四种NSAID的相对抗伤害感受作用与抗炎活性（通过抑制角叉菜胶诱导的大鼠爪水肿测定）之间缺乏相关性表明，它们的疼痛缓解特性可能不完全是它们的抗炎作用的结果。这些实验数据支持6-MNA作为炎性疼痛条件下的镇痛剂的治疗价值。
The antinociceptive activity of intramuscular 6-methoxy-2-naphthylacetic acid (6-MNA), the active metabolite of nabumetone, was examined in a rat model of unilateral hindpaw inflammation/hyperalgesia and compared with that of three other non-steroidal anti-inflammatory drugs (NSAIDs) - diclofenac, naproxen and piroxicam. Over a dose range of 10-100 mg/kg i.m., 6-MNA produced a dose-dependent increase in the withdrawal threshold to a noxious mechanical stimulus applied to the inflamed paw; however, a higher dose (300 mg/kg) produced no further increase in antinociceptive activity. Peak effects occurred 30 min after intramuscular injection. Diclofenac, naproxen and piroxicam produced antinociceptive effects that were qualitatively similar to those of 6-MNA. There was an indication of quantitative differences between the four NSAIDs in terms of potency and efficacy although this was not statistically significant. The rapid onset of effect and the lack of correlation between the relative antinociceptive effects of the four NSAIDs and the anti-inflammatory activities (assayed as inhibition of carrageenan-induced rat paw oedema) suggest that their pain relieving properties may not be entirely the result of their anti-inflammatory effects. These experimental data support the therapeutic value of 6-MNA as an analgesic in conditions of inflammatory pain.