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螺佐呋酮(AG - 629)可增加犬胃黏膜血流量:其抗溃疡作用的一种可能机制。

Spizofurone (AG-629) increases gastric mucosal blood flow in dogs: a possible mechanism of its anti-ulcer effect.

作者信息

Inatomi N, Satoh H, Nagaya H, Maki Y

出版信息

Eur J Pharmacol. 1985 Apr 16;110(3):343-50. doi: 10.1016/0014-2999(85)90562-x.

Abstract

The effect of spizofurone (AG-629), a new anti-ulcer agent, on gastric mucosal blood flow was investigated in anesthetized dogs and the effects were compared with those of prostaglandin E2. Intravenous administration of spizofurone in doses of 15 and 30 mg/kg caused a dose-related increase in gastric mucosal blood flow. Spizofurone (1-10 mg/ml) given intragastrically for 15 min produced a sustained increase in gastric mucosal blood flow in a concentration-dependent manner; with 3 mg/ml there was about a 50% increase in gastric mucosal blood flow at the peak and a 2 h duration of action. The mode of action of spizofurone was similar to that of prostaglandin E2. The reduction in the gastric mucosal blood flow as induced by indomethacin was markedly improved by spizofurone. The topical action of spizofurone was confirmed in an in situ experiment using a stomach flap fixed to a lucite chamber. These results indicate that spizofurone increases gastric mucosal blood flow after systemic and topical administration, and this increase in gastric mucosal blood flow would account for the anti-ulcer effects of this drug.

摘要

研究了新型抗溃疡药物螺佐呋酮(AG - 629)对麻醉犬胃黏膜血流的影响,并将其与前列腺素E2的作用进行了比较。静脉注射15和30mg/kg剂量的螺佐呋酮可引起胃黏膜血流呈剂量依赖性增加。胃内给予1 - 10mg/ml的螺佐呋酮15分钟,可使胃黏膜血流以浓度依赖性方式持续增加;给予3mg/ml时,胃黏膜血流峰值增加约50%,作用持续2小时。螺佐呋酮的作用方式与前列腺素E2相似。螺佐呋酮可显著改善吲哚美辛所致的胃黏膜血流减少。在使用固定于透明塑料腔室的胃瓣进行的原位实验中证实了螺佐呋酮的局部作用。这些结果表明,螺佐呋酮经全身和局部给药后均可增加胃黏膜血流,而这种胃黏膜血流的增加可能是该药物抗溃疡作用的原因。

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