The endogenous fatty acid ethanolamide, palmitylethanolamide, alleviated, in a dose-dependent manner, pain behaviors elicited in mice by injections of formalin (5%, intraplantar), acetic acid (0.6%, 0.5 ml per animal, intraperitoneal, i.p.), kaolin (2.5 mg per animal, i.p.), and magnesium sulfate (120 mg per kg, i.p.). The antinociceptive effects of palmitylethanolamide were prevented by the cannabinoid CB2 receptor antagonist SR144528 [N-([1s]-endo-1.3.3-trimethylbicyclo[2.3.1]heptan-2-yl)-5-(4-chloro-3-methylphenyl)-1-(4-methylbenzyl)-pyrazole-3-carboxamide], not by the cannabinoid CB1 receptor antagonist SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H-pyrazole-3-carboxamide x HCl]. By contrast, palmitylethanolamide had no effect on capsaicin-evoked pain behavior or thermal nociception. The endogenous cannabinoid, anandamide (arachidonylethanolamide), alleviated nociception in all tests (formalin, acetic acid, kaolin, magnesium sulfate, capsaicin and hot plate). These effects were prevented by the cannabinoid CB1 receptor antagonist SR141716A, not the cannabinoid CB2 receptor antagonist SR141716A. Additional fatty acid ethanolamides (oleylethanolamide, myristylethanolamide, palmitoleylethanolamide, palmitelaidylethanolamide) had little or no effect on formalin-evoked pain behavior, and were not investigated in other pain models. These results support the hypothesis that endogenous palmitylethanolamide participates in the intrinsic control of pain initiation. They also suggest that the putative receptor site activated by palmitylethanolamide may provide a novel target for peripherally acting analgesic drugs.

译文

内源性脂肪酸乙醇酰胺 (palmitylethanolamide) 以剂量依赖性方式减轻了通过注射福尔马林 (5%,足底内),乙酸 (0.6%,每只动物0.5毫升,腹膜内,腹腔内),高岭土 (每只动物2.5 mg,i.p.) 和硫酸镁 (120 mg/kg,i.p.)。大麻素CB2受体拮抗剂SR144528 [N-([1s]-endo-1.3.3-trimethylbicyclo[2.3.1]heptan-2-yl)-5-(4-氯-3-甲基苯基)-1-(4-甲基苄基)-pyrazole-3-carboxamide],非大麻素CB1受体拮抗剂SR141716A [N-(piperidin-1-yl)-5-(4-氯苯基)-1-(2,4-二氯苯基)-4-甲基-1h-吡唑-3-甲酰胺xhcl]。相比之下,棕榈乙醇酰胺对辣椒素引起的疼痛行为或热伤害感受没有影响。在所有测试 (福尔马林,乙酸,高岭土,硫酸镁,辣椒素和热板) 中,内源性大麻素,anandamide (花生四烯乙醇酰胺) 减轻了伤害性。大麻素CB1受体拮抗剂SR141716A,而不是大麻素CB2受体拮抗剂SR141716A预防了这些作用。额外的脂肪酸乙醇酰胺 (油酰乙醇酰胺,肉豆蔻乙醇酰胺,棕榈油酰乙醇酰胺,棕榈油酰乙醇酰胺) 对福尔马林诱发的疼痛行为几乎没有影响,也没有在其他疼痛模型中进行研究。这些结果支持内源性棕榈酰乙醇酰胺参与疼痛起始的内在控制的假设。他们还表明,由棕榈酰乙醇酰胺激活的推定受体位点可能为外周镇痛药物提供了新的靶标。

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