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首页> 外文期刊>Dhaka University Journal of Pharmaceutical Sciences >Analgesic Activities of Synthesized Divalent Metal Complexes of Tolfenamic Acid
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Analgesic Activities of Synthesized Divalent Metal Complexes of Tolfenamic Acid

机译:甲苯磺酸的合成二价金属配合物的镇痛活性

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The objective of the study was to synthesize and to uncover the potentially interesting biological peripheral and central analgesic activities of some new divalent metal complexes of tolfenamic acid. The inception of the study was carried out with the formation of complexes [Cu(tolf)2(H2O)]2, [Co(tolf)2(H2O)2] and [Zn(tolf)2(H2O)] through the reaction of tolfenamic acid, a potent anti-inflammatory drug, with Cu, Co and Zn salts. Characterization of the metal complexes of tolfenamic acid was furnished with spectral (FTIR, UV-Visible) and calorimetric (DSC) analysis. The peripheral analgesic activities of the complexes were investigated by acetic acid-induced writhing method. In peripheral analgesia model, Cu, Co and Zn complexes of tolfenamic acid showed significantly promising analgesic potency at a dose of 25 mg/kg body weight with percentage of inhibition of acetic acid induced writhing by 49.67% (p < 0.01), 67.32% (p < 0.001) and 72.55% (p < 0.001), respectively compared to the standard tolfenamic acid 46.41%. Radiant heat tail-flick test was used to observe the central analgesic activity which showed analgesic effect evidenced by % elongation time (34.59%, 25.34% and 53.08%), respectively compared to that of morphine 2 mg/kg body weight at an equimolar dose of tolfenamic acid at 10 mg/kg body weight after 30 minutes. In the final analysis, it can be stipulated that newly synthesized stable metal complexes of tolfenamic acid have promising pharmacological effects like peripheral and central analgesic potency. Therefore, these complexes may be the better therapeutic options in the near future however it needs further extensive analysis in the pharmacokinetics, pharmacodynamics and toxicology perspective.Dhaka Univ. J. Pharm. Sci. 15(1): 89-96, 2016 (June)
机译:这项研究的目的是合成和发现潜在的有趣的甲苯磺酸新的二价金属配合物的生物外围和中央镇痛活性。该研究的开始是通过反应形成配合物[Cu(tolf)2(H2O)] 2,[Co(tolf)2(H2O)2]和[Zn(tolf)2(H2O)]。甲苯磺酸,一种有效的消炎药,含铜,钴和锌盐。通过光谱(FTIR,UV-可见)和量热(DSC)分析提供了对甲苯磺酸的金属配合物的表征。用乙酸诱导的扭体法研究了复合物的外周镇痛活性。在周围镇痛模型中,甲苯磺酸的铜,钴和锌复合物在剂量为25 mg / kg体重时显示出非常有希望的镇痛效果,其中乙酸诱导的扭体抑制百分比为49.67%(p <0.01),67.32%( p <0.001)和72.55%(p <0.001),而标准的托芬那酸为46.41%。用放射热甩尾试验观察中枢镇痛作用,该镇痛作用由%延长时间(分别为34.59%,25.34%和53.08%)与等摩尔剂量的吗啡2 mg / kg体重相比证明。 30分钟后,服用10 mg / kg体重的托芬那酸。归根结底,可以规定新合成的托芬那酸稳定金属配合物具有良好的药理作用,如外周和中枢镇痛药效。因此,这些复合物在不久的将来可能是更好的治疗选择,但是需要在药代动力学,药效学和毒理学方面进行进一步的广泛分析。 J.药物科学15(1):89-96,2016(六月)

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