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酯化抗炎药莫尼氟酯的胃保护作用

Gastroprotective effects of morniflumate, an esterified anti-inflammatory drug.

作者信息

Schiantarelli P, Cadel S, Folco G C

出版信息

Arzneimittelforschung. 1984;34(8):885-90.

PMID:6333880
Abstract

An experimental study on morniflumate, the beta-morpholinoethyl ester of niflumic acid, was undertaken in the rat to test its gastroprotective and "cytoprotective" properties and to assess its effects on gastric secretion and on the prostaglandin contents in the stomach wall. Morniflumate induced intense and usually dose-dependent inhibition of the gastric hemorrhagic lesions caused by acetylsalicylic acid, indomethacin, diclofenac, ketoprofen, naproxen and phenylbutazone and of the gastric necrotic lesions caused by absolute ethanol, HCl 0.6 mol l-1, NaOH 0.2 mol l-1 and NaCl 25%. Morniflumate also exerted marked inhibition of gastric acid secretion both in normal and in pylorus-ligated rats. The compound raised the concentration of "cytoprotective" prostaglandins in the glandular portion of the stomach but did not reverse the synthesis-block effect of the ulcerogenic nonsteroidal anti-inflammatory drugs whose gastric effects it inhibited.

摘要

对尼氟酸的β-吗啉代乙酯莫尼氟酯进行了大鼠实验研究,以测试其胃保护和“细胞保护”特性,并评估其对胃分泌及胃壁中前列腺素含量的影响。莫尼氟酯对乙酰水杨酸、吲哚美辛、双氯芬酸、酮洛芬、萘普生和保泰松所致的胃出血性损伤以及无水乙醇、0.6 mol/L盐酸、0.2 mol/L氢氧化钠和25%氯化钠所致的胃坏死性损伤均有强烈且通常呈剂量依赖性的抑制作用。莫尼氟酯对正常大鼠和幽门结扎大鼠的胃酸分泌也有显著抑制作用。该化合物可提高胃腺部“细胞保护”前列腺素的浓度,但不能逆转致溃疡非甾体抗炎药的合成阻断效应,尽管它能抑制这些药物的胃效应。

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