Exploring the Anti-Inflammatory Effects of Aprepitant: An Antagonist of the Neurokinin-1 Receptor

Pavithra Pavithra J, Shila Shila G, Maheshwaran Maheshwaran P, John Staines M, Sakthi Sundaram S
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Abstract

Aim: Aim: Substance P participates towards pain aetiology by activating on the NK-1R, the neurokinin-1 receptor, which is found on sensory neurons that perceive noxious stimuli. SP is recognised to have biological action through G-protein-coupled neurokinin receptors named Neurokinin 1 Receptor (NK-1R), Neurokinin 2 Receptor (NK-2R) and neurokinin 3 receptors (NK-3R). Among the three, NK-1R has the highest affinity for substance P. The NK-1R receptor is a G-protein-coupled receptor that is involved in inflammatory disorders. Aprepitant is a highly selective non-peptide neurokinin-1 receptor antagonist that is approved to lessen nausea and vomiting brought on by chemotherapy. Materials and Methods: Materials and Methods: The purpose of this study is to see if Aprepitant has any anti-inflammatory activity in the cotton pellet granuloma technique. Pellets with granuloma tissue around them were carefully dissected, cleared of extraneous tissues, and dried at 60ºC at the end of the research. Under both moist and dry circumstances, and each particle’s surrounding granuloma tissue’s mean weight was determined. Results: Results: The study’s goal is to evaluate the anti-inflammatory impact and Aprepitant prevents granuloma formation (48.68%) at a dose of 80 mg/kg to the conventional medicine indomethacin (2.5 mg/kg), which demonstrated the maximum suppression of granuloma tissue development (55.34%). Conclusion: Conclusion: When compared to a control without an ulcerogenic impact, the histology of granuloma in aprepitant treated group tissue indicated considerable prevention of necrosis and exudates.
探索阿瑞匹坦的抗炎作用:一种神经激肽-1 受体拮抗剂
目的:目的:物质 P 通过激活神经激肽-1 受体 NK-1R(存在于感知有害刺激的感觉神经元上)参与疼痛病因学研究。SP 被认为是通过 G 蛋白偶联神经激肽受体(神经激肽 1 受体,NK-1R)、神经激肽 2 受体(NK-2R)和神经激肽 3 受体(NK-3R)发挥生物作用的。NK-1R 受体是一种 G 蛋白偶联受体,与炎症性疾病有关。阿瑞匹坦是一种高选择性非肽类神经激肽-1 受体拮抗剂,已被批准用于减轻化疗引起的恶心和呕吐。材料与方法材料与方法:本研究的目的是观察阿普瑞坦在棉球肉芽肿技术中是否具有抗炎活性。在研究结束时,仔细剖开周围带有肉芽肿组织的棉球,清除无关组织,并在 60ºC 温度下烘干。在潮湿和干燥的情况下,测定每个颗粒周围肉芽肿组织的平均重量。结果结果:结果:该研究的目的是评估抗炎效果,阿普瑞坦在剂量为 80 毫克/千克时可防止肉芽肿形成(48.68%),而传统药物吲哚美辛(2.5 毫克/千克)则表现出最大程度的抑制肉芽肿组织发展(55.34%)。结论结论与没有产生溃疡影响的对照组相比,阿普瑞坦治疗组肉芽肿组织的组织学显示,坏死和渗出得到了很大程度的预防。
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