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参与小鼠内脏痛中右旋酮洛芬镇痛的受体。

Receptors involved in dexketoprofen analgesia in murine visceral pain.

机构信息

Cardiovascular Department, Clinical Hospital, Universidad de Chile, Santiago, Chile.

出版信息

J Biosci. 2020;45.

Abstract

Various animal models, especially rodents, are used to study pain, due to the difficulty of studying it in humans. Many drugs that produce analgesia have been studied and there is evidence among which NSAIDs deserve to be highlighted. Dexketoprofen (DEX) provides a broad antinociceptive profile in different types of pain; therefore, this study was designed to evaluate the profile of antinociceptive potency in mice. Analgesic activity was evaluated using the acetic acid abdominal constriction test (writhing test), a chemical model of visceral pain. Dose-response curves for i.p. DEX administration (1, 3, 10, 30 and 100 mg/kg), using at least six mice in each of at least five doses, was obtained before and 30 min after pre-treatment with different pharmacological agents. Pretreatment of the mice with opioid receptor antagonists was not effective; however, the serotonin receptor antagonist and nitric oxide synthase inhibitor produce a significant increase in DEX-induced antinociception. The data from the present study shows that DEX produces antinociception in the chemical twisting test of mice, which is explained with difficulty by the simple inhibition of COX. This effect appears to be mediated by other mechanisms in which the contribution of the NO and 5-HT pathways has an important effect on DEXinduced antinociception.

摘要

各种动物模型,特别是啮齿类动物,被用于研究疼痛,因为在人类中研究疼痛具有挑战性。已经研究了许多产生镇痛作用的药物,其中非甾体抗炎药(NSAIDs)值得特别关注。右旋酮洛芬(DEX)在不同类型的疼痛中表现出广泛的镇痛作用;因此,本研究旨在评估 DEX 在小鼠中的镇痛效力谱。使用醋酸腹部收缩试验(扭体试验)评估镇痛活性,这是一种内脏疼痛的化学模型。在使用至少六只小鼠进行至少五个剂量的预处理之前和之后,获得了腹腔内给予 DEX(1、3、10、30 和 100 mg/kg)的剂量-反应曲线,使用不同的药理学药物进行预处理。阿片受体拮抗剂预处理对 DEX 没有效果;然而,5-羟色胺受体拮抗剂和一氧化氮合酶抑制剂可显著增加 DEX 诱导的镇痛作用。本研究的数据表明,DEX 在小鼠的化学扭体试验中产生镇痛作用,这很难用 COX 的简单抑制来解释。这种作用似乎通过其他机制介导,其中 NO 和 5-HT 途径的贡献对 DEX 诱导的镇痛作用具有重要影响。

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