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AHR - 5850:一种强效抗炎化合物。

AHR-5850: a potent anti-inflammatory compound.

作者信息

Sancilio L F, Reese D L, Cheung S, Alphin R S

出版信息

Agents Actions. 1977 Mar;7(1):133-44. doi: 10.1007/BF01964911.

Abstract

AHR-5850 is a non-steroidal anti-inflammatory compound possessing antipyretic and analgesic properties. AHR-5850 was 16.4 and 22.8 times more potent than phenylbutazone in suppressing acute (Evans blue-carrageenan pleural effusion) and chronic (adjuvant-induced arthritis) inflammation, respectively. The analgesic activity of AHR 5850 was 43 times that of acetylsalicylic acid in the Randall-Selitto assay, and 156 and 56.3 times more potent than phenylbutazone in the acetylcholine-induced abdominal constriction in mice and in the bradykinin-induced nociceptive response in dogs, respectively. Single-dose studies showed that AHR-5850 produced less gastric irritation than acetylsalicylic acid when applied topically to the exposed gastric mucosa of cats or when administered orally to rats and dogs. Upon subchronic oral administration to rats, the therapeutic ratio of AHR-5850 was twice that of phenylbutazone. This was based on the ratio of its potency relative to phenylbutazone in producing intestinal lesions to its anti-inflammatory potency relative to phenylbutazone in the adjuvant-induced arthritis.

摘要

AHR - 5850是一种具有解热和镇痛特性的非甾体抗炎化合物。在抑制急性(伊文思蓝 - 角叉菜胶性胸腔积液)和慢性(佐剂性关节炎)炎症方面,AHR - 5850分别比保泰松强16.4倍和22.8倍。在兰德尔 - 塞利托试验中,AHR 5850的镇痛活性是阿司匹林的43倍,在小鼠乙酰胆碱诱导的腹部收缩试验和犬缓激肽诱导的伤害性反应试验中,分别比保泰松强156倍和56.3倍。单剂量研究表明,当局部应用于猫暴露的胃黏膜或口服给予大鼠和犬时,AHR - 5850引起的胃刺激比阿司匹林少。对大鼠进行亚慢性口服给药时,AHR - 5850的治疗指数是保泰松的两倍。这是基于其在产生肠道病变方面相对于保泰松的效力与其在佐剂性关节炎中相对于保泰松的抗炎效力之比。

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