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首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Subanalgesic doses of dexketoprofen and HCT-2037 (nitrodexketoprofen) enhance fentanyl antinociception in monoarthritic rats.
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Subanalgesic doses of dexketoprofen and HCT-2037 (nitrodexketoprofen) enhance fentanyl antinociception in monoarthritic rats.

机译：亚镇痛剂量的右酮洛芬和HCT-2037（硝基右酮洛芬）可增强单关节炎大鼠的芬太尼镇痛作用。

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Subanalgesic doses of the non-steroidal antiinflammatory drugs (NSAID) dexketoprofen trometamol and nitroparacetamol (NCX-701) enhance mu-opiate fentanyl effect in acute nociception. It is not known if a similar combination of drugs is effective in situations of spinal cord sensitization. The aim of this study was to assess if the enhancement of fentanyl antinociception can be observed in carrageenan-induced monoarthritis, when combined with dexketoprofen (DKT) or nitrodexketoprofen (HCT-2037). Withdrawal reflexes were recorded as single motor units in male Wistar rats anesthetized with alpha-chloralose. Fentanyl was studied alone and in the presence of 0.4, 0.8 micromol/kg of DKT or 0.3 micromol/kg of HCT-2037. In responses to noxious mechanical stimulation, the ID50 of fentanyl was enhanced twofold by 0.8 micromol/kg DKT and more than fourfold by HCT-2037 and no significant recovery was observed 45 min later. DKT 0.4 micromol/kg was, however, very little effective. The opioid antagonist naloxone did not reverse the effect. Enhancement of fentanyl effect on wind-up was only observed with HCT-2037 but not with DKT. We conclude that the combined administration of subanalgesic doses of dexketoprofen derivatives, specially its nitroderivative, and the mu-opiate fentanyl is an effective antinociceptive therapy in situations of articular inflammation involving a naloxone-independent mechanism of action.
机译：亚镇痛剂量的非甾体抗炎药（NSAID）右酮洛芬特罗美他莫和硝基对乙酰氨基酚（NCX-701）可增强阿片芬太尼在急性伤害感受中的作用。尚不清楚类似的药物组合在脊髓致敏情况下是否有效。这项研究的目的是评估当与右酮洛芬（DKT）或硝基右酮洛芬（HCT-2037）联合使用时，在角叉菜胶诱发的单关节炎中是否能观察到芬太尼抗伤害感受的增强。退出反射被记录为在雄性Wistar大鼠中以α-氯醛糖麻醉后的单个运动单位。单独研究芬太尼并在0.4、0.8 micromol / kg的DKT或0.3 micromol / kg的HCT-2037的存在下进行研究。在对有害机械刺激的反应中，芬太尼的ID50升高了0.8 micromol / kg DKT，提高了两倍，而HCT-2037则提高了四倍以上，并且45分钟后未见明显恢复。但是，DKT 0.4 micromol / kg效果不佳。阿片拮抗剂纳洛酮没有逆转该作用。仅在HCT-2037中观察到芬太尼对缠绕的作用增强，而在DKT中未观察到。我们得出的结论是，在涉及纳洛酮非依赖性作用机制的关节炎症情况下，联合使用亚镇痛剂量的右酮洛芬衍生物（尤其是其硝基衍生物）和阿片芬太尼是一种有效的抗伤害感受疗法。

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