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替诺昔康(Ro 12 - 0068),一种新型非甾体抗炎药的药理和生化活性。

Pharmacological and biochemical activities of tenoxicam (Ro 12-0068), a new non-steroidal anti-inflammatory drug.

作者信息

Bradshaw D, Cashin C H, Kennedy A J, Roberts N A

出版信息

Agents Actions. 1984 Dec;15(5-6):569-77. doi: 10.1007/BF01966776.

Abstract

Tenoxicam, a new non-steroidal anti-inflammatory drug has been compared with piroxicam and indomethacin in a range of pharmacological and biochemical inflammation test systems. In a chronic (17-day) adjuvant arthritis in the rat, tenoxicam and piroxicam were equally effective in reducing several indices of inflammation and were less ulcerogenic and better tolerated than indomethacin. The oxicams reduced the oedematous and cellular components of a carrageenan pleurisy at 4 hours while at 24 hours they increased exudate volume and selectively inhibited the accumulation of mononuclear cells. These agents also reduced the inflammatory component of a delayed hypersensitivity response to methylated bovine serum albumin in the mouse. The oxicams were about 100-fold less active than indomethacin as inhibitors of prostaglandin synthetase but all three compounds reduced about equally the release of prostaglandin E2 from phagocytosing rat PMN and interleukin 1-stimulated human rheumatoid synovial cells. The compounds had no effect on the release of superoxide anion, lysosomal enzymes or collagenase from cultured cells, neither did they inhibit isolated collagenase. Only indomethacin stabilized albumin against heat denaturation.

摘要

替诺昔康是一种新型非甾体抗炎药,已在一系列药理学和生物化学炎症测试系统中与吡罗昔康和吲哚美辛进行了比较。在大鼠慢性(17天)佐剂性关节炎中,替诺昔康和吡罗昔康在减轻多种炎症指标方面效果相当,且比吲哚美辛的致溃疡作用更小,耐受性更好。在4小时时,昔康类药物可减轻角叉菜胶性胸膜炎的水肿和细胞成分,而在24小时时,它们会增加渗出液体积,并选择性抑制单核细胞的积聚。这些药物还可减轻小鼠对甲基化牛血清白蛋白迟发型超敏反应的炎症成分。作为前列腺素合成酶抑制剂,昔康类药物的活性比吲哚美辛低约100倍,但这三种化合物在减少吞噬大鼠中性粒细胞和白细胞介素1刺激的人类风湿滑膜细胞中前列腺素E2的释放方面效果大致相同。这些化合物对培养细胞中超氧阴离子、溶酶体酶或胶原酶的释放没有影响,也不抑制分离的胶原酶。只有吲哚美辛能使白蛋白稳定,防止热变性。

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