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N-(2-羧基苯基)-4-苯氧基乙酰胺某些衍生物的药理性质

Pharmacologic properties of some derivatives of N-(2-carboxyphenyl)-4-phenoxyacetamide.

作者信息

Cebo B, Krupińska J, Mazur J

出版信息

Arch Immunol Ther Exp (Warsz). 1979;27(3):415-24.

PMID:314282
Abstract

Three new inhibitors of prostaglandin (PG) synthetase: N-(2-carboxy-4-chlorophenyl)-phenoxyacetamide (ZR 29), N-(2-carobxy-4-chlorophenyl/-bromophenoxyacetamide (ZR-32), N-(2-carboxy-4-chlorophenyl)-4' - nitrophenoxyacetamide (ZR-35), in doses of 30-100-200 mg/kg p.o. inhibited edema in an acute inflammatory model, ZR-32 inhibited formation of granuloma. In the chronic inflammatory model, ZR-32 exerted strongest activity in the second and third weeks. ZR-32 demonstrated strong analgesic activity in the test of stimulation with electric current and in the "hot plate" test, besides antipyretic activity. Both compounds weekly irritated the gastric mucosa. In the tests applied, these compounds had no effect on the CNS. Their acute to toxicity was substantially lower than that of acetylsalicyclic aid and indomethacin.

摘要

三种新型前列腺素(PG)合成酶抑制剂:N-(2-羧基-4-氯苯基)-苯氧基乙酰胺(ZR 29)、N-(2-羧基-4-氯苯基)-溴苯氧基乙酰胺(ZR-32)、N-(2-羧基-4-氯苯基)-4'-硝基苯氧基乙酰胺(ZR-35),口服剂量为30-100-200mg/kg时,在急性炎症模型中可抑制水肿,ZR-32可抑制肉芽肿形成。在慢性炎症模型中,ZR-32在第二和第三周表现出最强活性。ZR-32除具有解热活性外,在电流刺激试验和“热板”试验中还表现出强烈的镇痛活性。这两种化合物每周都会刺激胃黏膜。在所进行的试验中,这些化合物对中枢神经系统无影响。它们的急性毒性远低于乙酰水杨酸和吲哚美辛。

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