基于白鼠甲醛水肿模型的 4.5-二氢异恶唑-5-甲酰胺(PAR-2 抑制剂)抗炎活性筛选

Q3 Pharmacology, Toxicology and Pharmaceutics
Mikhail K. Korsakov, Vladimir N. Fedorov, Nikolay A. Smirnov, A. Shetnev, Olga V. Leonova, Nikita N. Volkhin, Aleksandr I. Andreyev
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引用次数: 0

摘要

简介类风湿性关节炎(RА)是一种免疫炎症性疾病,全球发病率高达 1.0%。治疗类风湿关节炎的标准药物是基本药物、糖皮质激素和非类固醇抗炎药物,这些药物往往只能缓解或阻碍疾病的进程,不能彻底治愈患者。此外,平均有 20%-50%的患者对治疗无反应、对处方药过敏或发现药物无效。因此,人们正在广泛研究具有不同作用机制的药物,其中包括蛋白酶激活受体(PAR-2)拮抗剂。 材料与方法:通过在左脚后部肌腱下注射体积为 0.1 mL 的 2% 中性福尔马林溶液来再现炎症过程。实验共使用了 84 只白鼠。双氯芬酸钠作为参照药物。 结果与讨论研究 4.5-二氢异噁唑-5-甲酰胺的 5 种衍生物样本对大鼠福尔马林水肿发展的影响的实验表明,与其他研究物质相比,化合物 R001 的疗效开始较晚;只有在引入 R005、R004 和 R002 后,足部体积才会恢复到初始水平。与其他化合物相比,R005 能在更大程度上防止水肿的发展,无论是胃内给药还是皮下注射,其疗效都优于双氯芬酸钠。 结论上述五种化合物都具有抗炎活性,但在定性和定量方面的光谱都不太明确。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Screening of anti-inflammatory activity of 4.5-dihydroisoxazol-5-carboxamide (PAR-2 inhibitors) based on formaldehyde oedema model among white lab rats
Introduction: Rheumatoid arthritis (RА) is an immune-inflammatory disease intrinsic to up to 1.0% of the world’s population. Standard drugs for RA therapy are basic medications, glucocorticoids and non-steroid anti-inflammatory drugs, which often only ease or hinder the course of disease, not curing the patient completely. Also, on the average 20-50 % of patients are unresponsive to treatment, allergic to the prescribed drugs or find them ineffective. That is why medications with a different mechanism of action are being widely researched, some of them being antagonists of proteinase-activated receptors (PAR-2). Materials and Methods: The inflammatory process was reproduced by injecting a 2% solution of neutral formalin in a volume of 0.1 mL under the aponeurosis of the posterior left foot. A total of 84 white rats were used in the experiment. Diclofenac sodium was administered as a reference drug. Results and Discussion: An experiment on researching the impact of 5 samples of derivatives of 4.5-dihydroisoxazol-5-carboxamide on formalin oedema development among rats showed that the compound R001, compared with other substances studied, differs in the late onset of the therapeutic effect when ingested; the restoration of the foot volume to the initial level occurs only after the introduction of R005, R004 and R002. R005 to a greater extent than other compounds prevents the development of edema and has greater therapeutic efficacy than diclofenac sodium both with intragastric administration and subcutaneous injection. Conclusion: All five compounds in question showed anti-inflammatory activity, with the spectrum not so unequivocal both in qualitative and quantitative values.
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来源期刊
Research Results in Pharmacology
Research Results in Pharmacology Medicine-Pharmacology (medical)
CiteScore
1.50
自引率
0.00%
发文量
32
审稿时长
12 weeks
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