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新型潜在抗过敏药物CI-922对体外花生四烯酸代谢的影响。

Effect of CI-922, a potential new antiallergy agent, on arachidonic acid metabolism in vitro.

作者信息

Boctor A M, Pugsley T A

出版信息

Inflammation. 1986 Dec;10(4):435-41. doi: 10.1007/BF00915827.

Abstract

CI-922 (3,7-dimethoxy-4-phenyl-N-1H-tetrazol-5-yl-4H-furo[3,2-b]indole-2- carboxamide, 1,2-ethanediamine, 2:1), an antiallergy compound, was tested for its effects on arachidonic acid metabolism, and its potency was compared to that of proxicromil, BW-755C, indomethacin, and nordihydroguaiaretic acid (NDGA). CI-922 was both a relatively potent and selective inhibitor of 5-HETE and LTB4 formation in human leukocytes, being equipotent to BW-755C and about four-fold more potent than proxicromil. However, CI-922 was rather weak in inhibiting the formation of PGE2 in bovine seminal vesicles. The parallel inhibition of 5-HETE and LTB4 formation by CI-922 suggests that either direct or indirect inhibition of the 5-lipoxygenase pathway may explain, at least in part, its antiallergy properties.

摘要

CI-922(3,7-二甲氧基-4-苯基-N-1H-四唑-5-基-4H-呋喃并[3,2-b]吲哚-2-甲酰胺,与1,2-乙二胺比例为2:1),一种抗过敏化合物,被测试了其对花生四烯酸代谢的影响,并将其效力与色甘酸、BW-755C、吲哚美辛和去甲二氢愈创木酸(NDGA)进行了比较。CI-922是人类白细胞中5-羟二十碳四烯酸(5-HETE)和白三烯B4(LTB4)形成的相对强效且有选择性的抑制剂,其效力与BW-755C相当,比色甘酸强约四倍。然而,CI-922在抑制牛精囊中前列腺素E2(PGE2)形成方面相当弱。CI-922对5-HETE和LTB4形成的平行抑制表明,对5-脂氧合酶途径的直接或间接抑制可能至少部分解释了其抗过敏特性。

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