Abstract

Objective

The leukotrienes are inflammatory mediators. In the present study, the analgesic role of local montelukast, a cysteinyl leukotriene receptor antagonist, and the possible involvement of L-arginine/NO/cGMP/K_ATP channel pathway and PPARγ receptors was assessed in the formalin test in rats.

Methods and results

The local administration of montelukast into the hind paw produced dose-related analgesia during both phases of the formalin test. Furthermore, pre-treatment with L-NAME, methylene blue, and glibenclamide prevented montelukast (10 μg/paw)-induced antinociception in both early and late phases of the test. Moreover, the local L-arginine and diazoxide before the sub-effective dose of montelukast (3 μg/paw) produced an analgesic effect. Also, local GW-9662 blocked antinociception induced by montelukast plus pioglitazone (10 μg/paw).

Conclusion

In conclusion, montelukast produced peripheral analgesia through PPARγ receptors and activation of the L-arginine/NO/cGMP/K_ATP channel pathway, with potential for a new topical analgesic drug.

中文翻译：

---

Montelukast 是一种半胱氨酰白三烯受体拮抗剂，通过 L-精氨酸/一氧化氮/环 GMP/KATP 通道途径和 PPARγ 受体在疼痛动物模型中发挥局部镇痛作用

 抽象的

 客观的

白三烯是炎症介质。在本研究中，在大鼠福尔马林试验中评估了局部孟鲁司特（一种半胱氨酰白三烯受体拮抗剂）的镇痛作用，以及 L-精氨酸/NO/cGMP/K _ATP通道通路和 PPARγ 受体的可能参与。

 方法和结果

在福尔马林试验的两个阶段中，将孟鲁司特局部施用到后爪中产生剂量相关的镇痛作用。此外，在测试的早期和后期阶段，用 L-NAME、亚甲蓝和格列本脲进行预处理可防止孟鲁司特（10 μg/爪）诱导的镇痛作用。此外，在亚有效剂量孟鲁司特（3μg/爪）之前局部L-精氨酸和二氮嗪产生镇痛作用。此外，本地 GW-9662 还可阻断孟鲁司特加吡格列酮（10 μg/爪）诱导的镇痛作用。

 结论

总之，孟鲁司特通过 PPARγ 受体和 L-精氨酸/NO/cGMP/K _ATP通道通路的激活产生外周镇痛，具有成为新型局部镇痛药物的潜力。