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苯恶洛芬(2-[4-氯苯基]-α-甲基-5-苯并恶唑乙酸),LRCL 3794的药理学,一种具有抗炎活性的新化合物,其抗炎活性显然与抑制前列腺素合成无关。

The pharmacology of benoxaprofen (2-[4-chlorophenyl]-alpha-methyl-5-benzoxazole acetic acid), LRCL 3794, a new compound with antiinflammatory activity apparently unrelated to inhibition of prostaglandin synthesis.

作者信息

Cashin C H, Dawson W, Kitchen E A

出版信息

J Pharm Pharmacol. 1977 Jun;29(6):330-6. doi: 10.1111/j.2042-7158.1977.tb11330.x.

Abstract

Benoxaprofen is a potent and long-acting anti-inflammatory and antipyretic compound. Its anti-inflammatory activity has been demonstrated in carrageenan-induced oedema, in cellulose pellet granuloma and in both developing and established adjuvant arthritis tests in rats. Its antipyretic activity is greater than either aspirin or paracetamol in tests inducing pyrexia with yeast of 'E' pyrogen in rats and rabbits. Benoxaprofen has analgesic activity in tests where pain is accompanied by inflammation but not in other experimental models of pain. The weak prostaglandin synthetase inhibiting properties of this compound differentiate it from other acid anti-inflammatory compounds. The low ulcerogenic potential of benoxaprofen seen in animal models may be related to its relative inability to inhibit PG synthetase.

摘要

苯恶洛芬是一种强效长效的抗炎和解热化合物。它的抗炎活性已在角叉菜胶诱导的水肿、纤维素颗粒肉芽肿以及大鼠的佐剂性关节炎早期和晚期试验中得到证实。在大鼠和兔子中用酵母或“E”热原诱导发热的试验中,其解热活性强于阿司匹林或对乙酰氨基酚。苯恶洛芬在伴有炎症的疼痛试验中具有镇痛活性,但在其他疼痛实验模型中则没有。该化合物较弱的前列腺素合成酶抑制特性使其有别于其他酸性抗炎化合物。在动物模型中观察到的苯恶洛芬较低的致溃疡潜力可能与其相对无法抑制前列腺素合成酶有关。

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