Suppr超能文献

新型非甾体抗炎药d-2-[4-(3-甲基-2-噻吩基)苯基]丙酸(M-5011)对大鼠和豚鼠的抗炎、镇痛及解热作用

Anti-inflammatory, analgesic and anti-pyretic effects of d-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid (M-5011), a new non-steroidal anti-inflammatory drug, in rats and guinea pigs.

作者信息

Kido H, Murakami N, Ito A, Kimura K, Kodera N, Doi T, Naruse T

机构信息

Research & Development Laboratories, Maruho Co., Ltd., Osaka, Japan.

出版信息

Jpn J Pharmacol. 1998 Jan;76(1):75-86. doi: 10.1254/jjp.76.75.

Abstract

Anti-inflammatory, analgesic and anti-pyretic effects of d-2-[4-(3-methyl-2-thienyl)phenyl]propionic acid (M-5011), a new non-steroidal anti-inflammatory drug (NSAID), were compared with those of indomethacin, diclofenac sodium and ketoprofen in rats and guinea pigs. Anti-inflammatory effect of M-5011 on ultraviolet-induced erythema in guinea pigs was 11.7 and 1.8 times more potent than that of indomethacin and ketoprofen, respectively. Inhibitory effect of M-5011 on carrageenin-induced paw edema was 2 and 1.5 times more potent than that of indomethacin and diclofenac sodium, respectively. Analgesic effect of M-5011 on dry yeast-induced hyperalgesia or adjuvant-induced arthritic pain was equipotent to that of indomethacin, diclofenac sodium or ketoprofen. Anti-pyretic effect of M-5011 on yeast-induced pyrexia in rats was 4.2 and 4.6 times more potent than that of indomethacin and ketoprofen, respectively. Inhibitory effect of M-5011 on prostaglandin E2 production in the exudate of air-pouch inflammation induced by carrageenin was 1.75 times more potent than that in the non-inflamed site (stomach). As a result, gastric ulcerogenic activity of M-5011 was half that of indomethacin in rat. These results suggest that M-5011 shows more potent anti-inflammatory and anti-pyretic effects and equipotent analgesic effect with low gastro-ulcerogenic activity compared with classical NSAIDs.

摘要

将新型非甾体抗炎药(NSAID)d-2-[4-(3-甲基-2-噻吩基)苯基]丙酸(M-5011)的抗炎、镇痛和解热作用与吲哚美辛、双氯芬酸钠和酮洛芬在大鼠和豚鼠体内的作用进行了比较。M-5011对豚鼠紫外线诱导红斑的抗炎作用分别比吲哚美辛和酮洛芬强11.7倍和1.8倍。M-5011对角叉菜胶诱导的爪肿胀的抑制作用分别比吲哚美辛和双氯芬酸钠强2倍和1.5倍。M-5011对干酵母诱导的痛觉过敏或佐剂诱导的关节炎疼痛的镇痛作用与吲哚美辛、双氯芬酸钠或酮洛芬相当。M-5011对大鼠酵母诱导发热的解热作用分别比吲哚美辛和酮洛芬强4.2倍和4.6倍。M-5011对角叉菜胶诱导的气囊肿炎症渗出物中前列腺素E2产生的抑制作用比在非炎症部位(胃)强1.75倍。结果,M-5011在大鼠中的致胃溃疡活性是吲哚美辛的一半。这些结果表明,与经典NSAIDs相比,M-5011具有更强的抗炎和解热作用、相当的镇痛作用以及较低的胃溃疡形成活性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验