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抗炎药吡啶基 - 联苯基 - 乙酰胺(二苯吡胺)的药理特性。

Pharmacological properties of the anti-inflammatory agent pyridyl-biphenylyl-acetamide (diphenpyramide).

作者信息

Caliari S, Alfieri L, Gervasi G B, Sangiovanni M P, Scrollini F

出版信息

Arzneimittelforschung. 1977;27(11):2086-93.

PMID:304726
Abstract

Pyridyl-biphenylyl-acetamide (diphenpyramide, Z-876) is a new bisphenylalcanoic derivative with marked anti-inflammatory, analgesic, antipyretic and uricosuric properties. It is more active than phenylbutazone in the adjuvant polyarthritis in the rat when given prophylactically or therapeutically. It is thrice as active as phenylbutazone and ten times as active as acetylsalicylic acid (ASA) on the carrageenin-induced edema of the hind-paw. Diphenpyramide is characterized by low acute toxicity and by weak ulcerogenic activity. On the carrageenin-induced edema the therapeutic index of diphenpyramide is 30 times higher than that of indometacin and the ratio between the ED50 and the UD50 (ulcerogenic dose in 50% of the treated rats) is 39 times higher than that of ASA.

摘要

吡啶基 - 联苯基 - 乙酰胺(二苯吡胺,Z - 876)是一种新型双苯链烷酸衍生物,具有显著的抗炎、镇痛、解热和促尿酸排泄特性。在大鼠佐剂性多关节炎中,预防性或治疗性给药时,它比保泰松更具活性。在角叉菜胶诱导的后爪水肿模型中,其活性是保泰松的三倍,是乙酰水杨酸(ASA)的十倍。二苯吡胺的特点是急性毒性低且致溃疡活性弱。在角叉菜胶诱导的水肿模型中,二苯吡胺的治疗指数比吲哚美辛高30倍,其半数有效剂量(ED50)与半数溃疡剂量(UD50,50%受试大鼠出现溃疡的剂量)之比比ASA高39倍。

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