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4-硝基-2-苯氧基甲磺酰苯胺(R-805):一种化学结构新颖的抗炎剂。

4-nitro-2-phenoxymethanesulfonanilide (R-805): a chemically novel anti-inflammatory agent.

作者信息

Swingle K F, Moore G G, Grant T J

出版信息

Arch Int Pharmacodyn Ther. 1976 May;221(1):132-9.

PMID:962423
Abstract

The anti-inflammatory activity of the sulfonanilide, 4-nitro-2-phenoxymethanesulfonanilide (R-805) has been demonstrated in conventional models (carrageenan-induced edema of the rat's paw, UV-induced erythema of guinea-pig skin, adjuvant-induced arthritis of the rat). R-805 differs from most currently available acidic anti-inflammatory drugs in that its functional acidic group is not carboxyl. The relative anti-inflammatory potency of R-805 is comparable to indomethacin. Calculation of acute therapeutic indices (LD50/ED50) for 8 acidic anti-inflammatory drugs show R-805 to possess a more favourable index than the other drugs examined.

摘要

磺胺苯胺类化合物4-硝基-2-苯氧基甲烷磺胺苯胺(R-805)的抗炎活性已在传统模型中得到证实(角叉菜胶诱导的大鼠足爪水肿、紫外线诱导的豚鼠皮肤红斑、佐剂诱导的大鼠关节炎)。R-805与目前大多数可用的酸性抗炎药物不同,其功能性酸性基团不是羧基。R-805的相对抗炎效力与吲哚美辛相当。对8种酸性抗炎药物的急性治疗指数(LD50/ED50)计算表明,R-805的指数比所检测的其他药物更有利。

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