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Comparison of the antinociceptive effects of ibuprofen arginate and ibuprofen in rat models of inflammatory and neuropathic pain

机译:精氨酸布洛芬和布洛芬在炎性和神经性疼痛大鼠模型中的镇痛作用比较

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Aims Ibuprofen arginate is a highly soluble salt formed by combining racemic ibuprofen with the amino acid l-arginine. This formulation is absorbed faster, and it is safe and effective in treating many forms of mild to moderate pain. We compared the analgesic effect of ibuprofen arginate and conventional ibuprofen in rat models of pain. Main methods Mechanical and cold allodynia were assessed in the chronic constriction injury (CCI) model of neuropathic pain, and mechanical allodynia was also examined in capsaicin-injected rats (a model of central sensitization). Inflammatory hypersensitivity was assessed with the formalin test. Ibuprofen-l-arginine, ibuprofen, l-arginine or saline was administered orally on a daily basis after CCI or capsaicin injection, and the von Frey and cold plate tests were performed on days 1, 3 and 7 after CCI or capsaicin administration. In the formalin-induced inflammatory pain test, the drugs were administered 30 min before formalin injection. Key findings Ibuprofen only exerts an antinociceptive effect in the formalin model whereas ibuprofen-l-arginine exerts antinociceptive effects on both mechanical and cold allodynia induced by CCI, mechanical allodynia induced by capsaicin injection, and in phase 2 of the formalin test, exhibiting superior antinociceptive activity to ibuprofen in all these tests. l-Arginine only exerted antinociceptive effects on cold allodynia in CCI. Significance These results demonstrate that ibuprofen arginate has stronger antinociceptive effects than ibuprofen in all the models used, suggesting it might improve the therapeutic management of neuropathic and inflammatory pain.
机译:目的是布洛芬精氨酸是通过将外消旋布洛芬与氨基酸1-精氨酸结合而形成的高度可溶的盐。该制剂吸收速度更快,在治疗多种形式的轻度至中度疼痛方面是安全有效的。我们比较了精氨酸布洛芬和常规布洛芬在大鼠疼痛模型中的镇痛作用。主要方法在神经性疼痛的慢性收缩性损伤(CCI)模型中评估了机械性和冷性异常性疼痛,还对注射了辣椒素的大鼠(中枢性敏化模型)进行了机械性异常性疼痛的检查。用福尔马林测试评估炎症性超敏反应。布洛芬-1-精氨酸,布洛芬,1-精氨酸或生理盐水在CCI或辣椒素注射后每天口服,在CCI或辣椒素施用后的第1、3和7天进行von Frey和冷板试验。在福尔马林诱导的炎性疼痛测试中,在福尔马林注射前30分钟给药。主要发现布洛芬仅在福尔马林模型中发挥镇痛作用,而布洛芬-1-精氨酸对CCI诱发的机械性和冷性异常性疼痛,辣椒素注射引起的机械性异常性疼痛以及福尔马林试验的第二阶段均具有镇痛作用。在所有这些测试中对布洛芬具有活性。 l-精氨酸仅对CCI中的冷异常性疼痛具有镇痛作用。意义这些结果表明,在所有使用的模型中,精氨酸布洛芬比布洛芬具有更强的镇痛作用,表明它可能改善神经性和炎性疼痛的治疗方法。

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