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一种非甾体抗炎药托美汀钠对实验动物渗出性炎症的作用(作者译)

[Effect of a non-steroidal anti-inflammatory agent, tolmetin sodium on exudative inflammation in experimental animals (author's transl)].

作者信息

Nakamura H, Yokoyama Y, Motoyoshi S, Ishii K, Shimizu M

出版信息

Nihon Yakurigaku Zasshi. 1979 Jul;75(5):447-58. doi: 10.1254/fpj.75.447.

Abstract

Effect of tolmetin sodium(Tol) on acute and subacute exudative inflammation was tested in experimental animals. Tol had a potent inhibitory activity (ED50 = 0.75 mg/kg, p.o.) on the increased vascular permeability induced by acetic acid in mice, and the potency was about 0.4 times that of indomethacin (Ind), and 6-93 times that of ibuprofen (Ibu), phenylbutazone(Phe) and aspirin(Asp). The inhibitory activity of Tol(ED50 = 18.2 mg/kg, p.o.) on UV-induced erythema in guinea pigs was about 0.3 times that of Ind. A recovery of the hind paw edema of rats, produced by a mixture of kaolin and carrageenin, was promoted by oral administration of Tol(2.5 approximately 20 mg/kg x 5/2 days). Tol(80 mg/kg/day, p.o.) showed a significant activity in inhibiting the exudation caused by croton oil in rats, and the activity was about 0.025 times that of Ind and greater than that of Ibu, Phe and Asp. Tol(100-800 microgram/ml) inhibited in a dose-dependent manner the phytohemagglutinin-induced blast transformation of cultured lymphocytes from rat thymus, as did salicylic acid. In vitro, Tol showed a potent activity similar to that of Ibu and Phe in preventing the denaturation of bovine serum albumin and the lysis of rat erythrocytes. From these results, it is suggested that Tol has a particularly potent inhibitory activity on acute exudative inflammation, and the mode of action may be attributed to a mechanism similar to that seen with other acidic non-steroidal anti-inflammatory drugs.

摘要

在实验动物中测试了托美丁钠(Tol)对急性和亚急性渗出性炎症的作用。Tol对小鼠醋酸诱导的血管通透性增加具有强效抑制活性(口服半数有效量ED50 = 0.75毫克/千克),其效力约为吲哚美辛(Ind)的0.4倍,布洛芬(Ibu)、保泰松(Phe)和阿司匹林(Asp)的6 - 93倍。Tol(口服半数有效量ED50 = 18.2毫克/千克)对豚鼠紫外线诱导的红斑的抑制活性约为Ind的0.3倍。口服给予Tol(2.5至20毫克/千克×5/2天)可促进高岭土和角叉菜胶混合物所致大鼠后爪水肿的消退。Tol(口服80毫克/千克/天)在抑制大鼠巴豆油引起的渗出方面具有显著活性,其活性约为Ind的0.025倍,大于Ibu、Phe和Asp。Tol(100 - 800微克/毫升)与水杨酸一样,以剂量依赖性方式抑制植物血凝素诱导的大鼠胸腺培养淋巴细胞的母细胞转化。在体外,Tol在防止牛血清白蛋白变性和大鼠红细胞溶解方面显示出与Ibu和Phe相似的强效活性。从这些结果表明,Tol对急性渗出性炎症具有特别强效的抑制活性,其作用方式可能归因于与其他酸性非甾体抗炎药类似的机制。

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