Silva Lívia Caroline Resende, Castor Marina Gomes Miranda E, Navarro Larissa Caldeira, Romero Thiago Roberto Lima, Duarte Igor Dimitri Gama
Department of Pharmacology, Institute of Biological Sciences, ICB-UFMG, Av. Antônio Carlos, 6627, Pampulha, CEP 31.270-100, Belo Horizonte, MG, Brazil.
Neurosci Lett. 2016 May 27;622:6-9. doi: 10.1016/j.neulet.2016.04.029. Epub 2016 Apr 14.
NSAIDs represent some of the most widely prescribed drugs for relief of short-term fever, pain and inflammation. The participation of the opioid system in the peripheral is poorly understood. The aim of this study was evaluate the role of opioid system in the peripheral antinociception by diclofenac and dipyrone. To test this hypothesis, opioid receptor antagonists were evaluated using the rat paw pressure test, in which pain sensitivity is increased by intraplantar injection of prostaglandin E2 (PGE2, 2μg). Diclofenac (20μg/paw) and Dipyrone (40μg/paw) administered locally into the right paw elicited an antinociceptive effect. It was used naloxone (50μg/paw), a non-selective opioid receptor antagonist, which antagonized peripheral antinociception induced by diclofenac and dipyrone. Selectively, it was evaluated the μ-, δ- and κ-opioid receptor antagonists, respectively, clocinnamox (40μg/paw), naltrindole (50μg/paw) and nor-binaltorphimine (20, 40 and 80μg/paw). Our data indicated that only the κ-opioid antagonist was capable to reverse the peripheral antinociception by NSAIDs. The present results provide evidence that the opioid system participated in the diclofenac and dipyrone-induced peripheral antinociception by indirect activation of κ-opioid receptor probable by release of endogenous opioids such as dynorphins.
非甾体抗炎药是用于缓解短期发热、疼痛和炎症的最广泛处方药物中的一部分。人们对阿片系统在外周的参与情况了解甚少。本研究的目的是评估阿片系统在双氯芬酸和安乃近外周抗伤害感受中的作用。为了验证这一假设,使用大鼠 paw 压力试验评估阿片受体拮抗剂,在该试验中,通过足底注射前列腺素 E2(PGE2,2μg)可增加疼痛敏感性。将双氯芬酸(20μg/爪)和安乃近(40μg/爪)局部注射到右爪可产生抗伤害感受作用。使用了非选择性阿片受体拮抗剂纳洛酮(50μg/爪),它拮抗了双氯芬酸和安乃近诱导的外周抗伤害感受。分别选择性地评估了 μ-、δ-和 κ-阿片受体拮抗剂,即氯辛肟(40μg/爪)、纳曲吲哚(50μg/爪)和去甲二氢吗啡酮(20、40 和 80μg/爪)。我们的数据表明,只有 κ-阿片拮抗剂能够逆转非甾体抗炎药的外周抗伤害感受。目前的结果提供了证据,表明阿片系统通过内源性阿片类物质如强啡肽的释放间接激活 κ-阿片受体参与了双氯芬酸和安乃近诱导的外周抗伤害感受。