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3-甲基-5-苯甲酰氨基异噻唑-4-羧酸对氯苯酰胺(化合物ITCL)的药理研究——最终抗炎作用的制备

Pharmacological studies on p-chlorophenylamide of 3-methyl-5-benzoylaminoizothiazole-4-carboxylic acid (compound ITCL) the preparation of eventual anti-inflammatory effect.

作者信息

Giełdanowski J, Kowalczyk-Bronisz S H, Machoń Z, Szary A, Błaszczyk B

出版信息

Arch Immunol Ther Exp (Warsz). 1980;28(3):393-407.

PMID:7447644
Abstract

Pharmacological activity of p-chlorophenylamide of 3-methyl-5-benzoylaminoizothiazole-4-carboxylic acid (compound ITCl) was studied with special regard to its anti-inflammatory effect. Compound ITCl is moderately toxic with no distinct circulatory and central effect. On the other hand, it shows strong anti-inflammatory activity in many tests of immunologically specific, nonspecific and infectious inflammations. The greatest efficacy of the compound was noted in the therapy of experimental, immunologically non-specific (xylene, carrageenin and cotton-test) inflammations. Weaker and less regular therapeutic effect was noted in the cases of immunologic inflammations -- mainly in contact reaction to dinitrochlorobenzene. Compound ITCl was ineffective in relation to transplantation barrier. Therapeutic efficacy of the compound was not observed in herpetic inflammation of the skin. On the other hand, a promising therapeutic effect was noticed in relation to cow-pox virus keratitis. Compound ITCl is well tolerated. It shows no toxic effect on white and red blood cells system in a 4-week exposition. Compound ITCl stabilizes cell membranes. Practical aspect of the obtained results was discussed.

摘要

研究了3-甲基-5-苯甲酰氨基异噻唑-4-羧酸对氯苯酰胺(化合物ITCl)的药理活性,特别关注其抗炎作用。化合物ITCl毒性中等,无明显的循环和中枢作用。另一方面,在许多免疫特异性、非特异性和感染性炎症试验中,它显示出强大的抗炎活性。该化合物在实验性免疫非特异性(二甲苯、角叉菜胶和棉球试验)炎症治疗中疗效最佳。在免疫性炎症病例中,观察到较弱且不太规律的治疗效果——主要是在对二硝基氯苯的接触反应中。化合物ITCl对移植屏障无效。在皮肤疱疹性炎症中未观察到该化合物的治疗效果。另一方面,在牛痘病毒性角膜炎方面观察到有前景的治疗效果。化合物ITCl耐受性良好。在4周的暴露实验中,它对白细胞和红细胞系统未显示出毒性作用。化合物ITCl可稳定细胞膜。讨论了所得结果的实际意义。

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