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FPL 62064,一种局部活性的5-脂氧合酶/环氧化酶抑制剂。

FPL 62064, a topically active 5-lipoxygenase/cyclooxygenase inhibitor.

作者信息

Blackham A, Griffiths R J, Hallam C, Mann J, Mitchell P D, Norris A A, Simpson W T

机构信息

Department of Biochemistry, Fisons plc-Pharmaecutical Division, Loughborough, Leicestershire, UK.

出版信息

Agents Actions. 1990 Jun;30(3-4):432-42. doi: 10.1007/BF01966309.

Abstract

FLP 62064 [N-(4-methoxyphenyl)-1-phenyl-1H-pyrazole-3-amine] is a dual inhibitor of prostaglandin synthetase and 5-lipoxygenase. The compound had anti-inflammatory activity in vivo in a number of models. It inhibited peritoneal inflammation induced by immune-complex when given locally. When applied to the skin, FPL 62064 inhibited UV irradiation-induced erythema and PGE2 formation in the guinea pig and also oedema formation and eicosanoid production in the mouse ear produced by arachidonic acid. Co-injected with arachidonic acid in rabbit skin, FPL 62064 inhibited oedema and eicosanoid formation.

摘要

FLP 62064 [N-(4-甲氧基苯基)-1-苯基-1H-吡唑-3-胺] 是一种前列腺素合成酶和5-脂氧合酶的双重抑制剂。该化合物在多种体内模型中具有抗炎活性。局部给药时,它能抑制免疫复合物诱导的腹膜炎症。将FPL 62064应用于皮肤时,可抑制豚鼠紫外线照射诱导的红斑和PGE2形成,以及花生四烯酸在小鼠耳中引起的水肿形成和类花生酸生成。在兔皮肤中与花生四烯酸共同注射时,FPL 62064可抑制水肿和类花生酸形成。

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