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前列腺素E2衍生物恩前列素(TA/RS-84135)的抗分泌作用:对蛙皮素刺激分泌的抑制作用

Antisecretory effect of a PGE2 derivative, enprostil (TA/RS-84135): inhibitory action of amogastrin-stimulated secretion.

作者信息

Kohli Y, Katoh T, Suzuki K

机构信息

Second Department of Internal Medicine, Fukui Medical School, Japan.

出版信息

Drugs Exp Clin Res. 1988;14(11):673-8.

PMID:3149933
Abstract

A newly developed prostaglandin E2 derivative, enprostil (TA/RS-84135), was administered to five healthy volunteers in the stomach and duodenum through a teflon tube to examine its effect on amogastrin-stimulated gastric acid secretion. The acid output 1-3 h after administration of enprostil (35 micrograms) decreased remarkably as compared with that in the same period after placebo administration. However, no significant difference in antisecretory effect was observed between the two routes of administration. A decrease in pepsin output occurred in parallel with the decrease in acid output. These results suggest that the antisecretory effect of enprostil is at least partially due to systemic absorption and the predominantly topical action seen in animals does not seem to occur in man. No side-effects attributable to enprostil were observed during the test period. In conclusion, enprostil seems to be clinically useful as an antiulcer agent.

摘要

一种新研制的前列腺素E2衍生物恩前列素(TA/RS - 84135),通过聚四氟乙烯管经胃和十二指肠给予5名健康志愿者,以研究其对胃泌素刺激的胃酸分泌的影响。给予恩前列素(35微克)后1 - 3小时的胃酸分泌量与给予安慰剂后同期相比显著下降。然而,两种给药途径的抗分泌作用未观察到显著差异。胃蛋白酶分泌量的减少与胃酸分泌量的减少同时发生。这些结果表明,恩前列素的抗分泌作用至少部分归因于全身吸收,在动物中所见的主要局部作用在人类中似乎并不发生。在试验期间未观察到归因于恩前列素的副作用。总之,恩前列素似乎作为一种抗溃疡药物在临床上是有用的。

相似文献

1
Antisecretory effect of a PGE2 derivative, enprostil (TA/RS-84135): inhibitory action of amogastrin-stimulated secretion.前列腺素E2衍生物恩前列素(TA/RS-84135)的抗分泌作用:对蛙皮素刺激分泌的抑制作用
Drugs Exp Clin Res. 1988;14(11):673-8.
2
Gastric antisecretory and antiulcer properties of enprostil, (+/-)-11 alpha, 15 alpha-dihydroxy-16-phenoxy-17,18,19,20-tetranor-9-oxoprosta- 4,5,13(t)-trienoic acid methyl ester.恩前列素((+/-)-11α,15α-二羟基-16-苯氧基-17,18,19,20-四降-9-氧代前列腺-4,5,13(t)-三烯酸甲酯)的胃抗分泌及抗溃疡特性
J Pharmacol Exp Ther. 1986 Nov;239(2):382-9.
3
Inhibitory action of enprostil (4,5-dehydro-16-phenoxy-17,18,19,20-tetranor-PGE2) on tetra-gastrin stimulated acid secretion in human subjects.恩前列素(4,5-脱氢-16-苯氧基-17,18,19,20-四去甲-PGE2)对人体四肽胃泌素刺激的胃酸分泌的抑制作用。
Gastroenterol Jpn. 1989 Apr;24(2):115-9. doi: 10.1007/BF02774184.
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Effect of trimoprostil on gastric secretion in man.曲莫前列素对人体胃液分泌的影响。
Arzneimittelforschung. 1988 Jun;38(6):833-9.
5
[Effects of enprostil on changes in the gastric transepithelial potential differential induced by aspirin].恩前列素对阿司匹林诱导的胃跨上皮电位差变化的影响
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6
Effect of a single oral dose of enprostil on gastric secretion and gastrin release. Studies in healthy volunteers and patients with pernicious anemia.单次口服恩前列素对胃酸分泌和胃泌素释放的影响。对健康志愿者和恶性贫血患者的研究。
Am J Med. 1986 Aug 18;81(2A):40-3. doi: 10.1016/s0002-9343(86)80009-2.
7
Effects of the natural and unnatural isomers and degradation products of enprostil on gastric acid secretion and gastrointestinal motility in the rat.恩前列素的天然和非天然异构体及降解产物对大鼠胃酸分泌和胃肠动力的影响。
Arzneimittelforschung. 1989 Dec;39(12):1568-71.
8
Enprostil, a synthetic prostaglandin E2 analogue, inhibits meal-stimulated gastric acid secretion and gastrin release in patients with duodenal ulcer.恩前列素,一种合成的前列腺素E2类似物,可抑制十二指肠溃疡患者进食刺激后的胃酸分泌和胃泌素释放。
Am J Med. 1986 Aug 18;81(2A):44-9. doi: 10.1016/s0002-9343(86)80010-9.
9
Sustained enhancement of gastric HCO3 secretion in humans by enprostil.恩前列素对人体胃碳酸氢盐分泌的持续增强作用。
Therapie. 1991 Jan-Feb;46(1):13-5.
10
Specificity of PGE2 analogs interaction between food intake and antisecretory effect.PGE2类似物在食物摄入与抗分泌作用之间相互作用的特异性。
Prostaglandins Leukot Med. 1986 Oct;24(2-3):219-25. doi: 10.1016/0262-1746(86)90129-0.