Pharmacodynamics and toxicology of fenflumizole, a new non-steroidal anti-inflammatory imidazole derivative.

T Corell, G Hasselmann
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引用次数: 21

Abstract

Fenflumizole, (2-(2,4-difluorophenyl)-4,5-bis(4-methoxyphenyl) imidazole), a new non-steroidal anti-inflammatory agent, was investigated for anti-inflammatory, analgesic and anti-pyretic activity in experimental animals. Comparison was made to other non-steroidal anti-phlogistics. Furthermore, general pharmacodynamics and toxicity of fenflumizole was studied. Fenflumizole was comparable to or weaker than indomethacin in models of acute inflammation (carrageenin paw oedema and pleurisy, rats, ultraviolet erythema, guinea-pigs) and stronger than indomethacin as an analgesic (writhing, mice). As an antipyretic agent (arachidonic acid pyresis, rats) fenflumizole was 3 times weaker than indomethacin. The acute gastro-ulcerogenicity and toxicity of fenflumizole was low as compared to reference drugs. No untoward activity of fenflumizole on respiratory and circulatory systems was observed in rabbits and dogs. Fenflumizole is a potential new therapeutic agent with anti-inflammatory, analgesic and anti-pyretic activities comparable to other anti-phlogistics but with reduced side effects.

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新型非甾体抗炎咪唑衍生物芬氟唑的药效学和毒理学研究。
研究了新型非甾体抗炎药芬氟唑(2-(2,4-二氟苯基)-4,5-双(4-甲氧基苯基)咪唑)在动物体内的抗炎、镇痛和解热作用。并与其他非甾体类抗炎药进行比较。此外,还研究了芬氟唑的一般药效学和毒性。在急性炎症模型(角叉菜胶足部水肿和胸膜炎,大鼠,紫外线红斑,豚鼠)中,芬氟唑与吲哚美辛相当或较弱,作为镇痛药(扭体,小鼠)比吲哚美辛强。作为退热剂(花生四烯酸退热,大鼠),芬氟唑比吲哚美辛弱3倍。与参比药物相比,芬氟唑的急性胃溃疡性和毒性较低。芬氟唑对家兔和狗的呼吸和循环系统均未见不良反应。芬氟唑是一种潜在的新型治疗药物,具有抗炎、镇痛和退热作用,与其他抗炎药相当,但副作用更小。
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