首页> 外文期刊>Pharmacology, Biochemistry and Behavior >Antinociceptive effect of 3-(4-fluorophenyl) -5 -trifluoromethyl- 1H-1-tosylpyrazole. A Celecoxib structural analog in models of pathological pain
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Antinociceptive effect of 3-(4-fluorophenyl) -5 -trifluoromethyl- 1H-1-tosylpyrazole. A Celecoxib structural analog in models of pathological pain

机译:3-(4-氟苯基)-5-三氟甲基-1H-1-甲苯磺酰基吡唑的镇痛作用。 Celecoxib结构类似物在病理性疼痛模型中的作用

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摘要

Pain is the most common complaint in the medical field and the identification of novel compounds that can effectively treat painful states without causing side effects remains a major challenge in biomedical research. The aim of the present study is to investigate the antinociceptive effect of 3-(4-fluorophenyl)-5-trifluoromethyl-1H-1 -tosylpyrazole (FTosPz) in models of pathological pain in mice and compare these effects with those produced by Celecoxib, FTosPz (100-500 umol/kg) or Celecoxib (26-260 urnol/kg) was administrated orally. The administration of either FTosPz or Celecoxib reduced the hyperalgesia but not the edema or leukocyte infiltration that was caused by Complete Freund's Adjuvant (CFA), used as an arthritis model. Oral administration of both FTosPz and Celecoxib also attenuated the postoperative hyperalgesia as well as the hyperalgesia caused by partial sciatic nerve ligation, used as a neuropathic pain model. FTosPz and Celecoxib produced antinociceptive effects without altering the locomotor activity of animals. Furthermore, FTosPz neither altered AST/ALT enzyme activity nor the urea/creatinine levels. Still, the FTosPz did not alter the COX-t and CGX-2 enzyme activities. Thus, FTosPz is an interesting prototype for the development of novel analgesic drugs.
机译:疼痛是医学领域最常见的主诉,并且能够有效治疗疼痛状态而不会引起副作用的新型化合物的鉴定仍然是生物医学研究中的主要挑战。本研究的目的是研究3-(4-氟苯基)-5-三氟甲基-1H-1-甲苯磺酰基吡唑(FTosPz)在小鼠病理性疼痛模型中的镇痛作用,并将这些作用与塞来昔布产生的作用进行比较,口服FTosPz(100-500 umol / kg)或Celecoxib(26-260 urnol / kg)。 FTosPz或Celecoxib的使用减少了痛觉过敏,但并未减轻由完全弗氏佐剂(CFA)引起的水肿或白细胞浸润,CFA是关节炎模型。口服FTosPz和Celecoxib还可以减轻术后痛觉过敏以及由局部坐骨神经结扎引起的痛觉过敏,用作神经性疼痛模型。 FTosPz和Celecoxib产生抗伤害作用,而不会改变动物的运动活性。此外,FTosPz既不改变AST / ALT酶的活性,也不改变尿素/肌酐的水平。尽管如此,FTosPz并没有改变COX-t和CGX-2酶的活性。因此,FTosPz是开发新型止痛药的有趣原型。

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