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15(R)-15-甲基前列腺素E2对人胃酸分泌的抑制作用及其与阿托品的相互作用。

The inhibitory effect of 15(R)15 methyl prostaglandin E2 and the interaction with atropine on stimulated gastric acid secretion in man.

作者信息

Kollberg B, Johansson C

出版信息

Scand J Gastroenterol. 1979;14(3):337-42. doi: 10.3109/00365527909179893.

Abstract

The inhibitory effect of 15(R)15 methyl prostaglandin E2 (Me PGE2) on the gastric acid response to pentagastrin stimulation, 0.6 micrograms.kg-1.h-1, was examined in healthy male volunteers. Each subject underwent a control test and tests with intragastrically administered graded doses of 15(R)15 Me PGE2 as free acid (80, 140, 200, and 400 micrograms, n = 5) and as methylester (80, 140, and 200 micrograms, n = 6). The percentage inhibition of the acid output during 2 h after increasing doses of the free acid was 24 +/- 11, 49 +/- 7, 44+/-9, and 76 +/- 12%. Corresponding figures for the methylester were 35 +/- 2, 54 +/- 5, and 64 +/- 8%. Both volume and acidity were reduced. Side effects did not occur, except for moderate diarrhoea in one subject after 400 micrograms of the free acid. In a third series (n = 6) the combined effect of 80 micrograms methyl ester (44 +/- 5% inhibition) and 1.5 mg atropine sulphate was studied. Atropine alone gave a 43 +/- 6% inhibition by lowering the secreted volumes. For the combination the inhibition was 82 +/- 3%. Intragastric 15(R)15 Me PGE2 inhibited dose-dependently the pentagastrin-stimulated gastric acid response. Differences between the free acid and methyl ester of the analogue were not significant. Compared with other Me PGE2 compounds, 15(R)15 Me PGE2 was less effective per dose, but the dose range was broader and side effects were slight. Concomitantly given atropine had a significant additive inhibitory effect.

摘要

在健康男性志愿者中研究了15(R)15-甲基前列腺素E2(Me PGE2)对五肽胃泌素刺激(0.6微克·千克-1·小时-1)引起的胃酸反应的抑制作用。每位受试者均接受了一次对照试验,以及用游离酸(80、140、200和400微克,n = 5)和甲酯(80、140和200微克,n = 6)经胃内给予不同剂量的15(R)15 Me PGE2的试验。游离酸剂量增加后2小时内胃酸分泌量的抑制百分比分别为24±11%、49±7%、44±9%和76±12%。甲酯的相应数字分别为35±2%、54±5%和64±8%。胃液量和酸度均降低。除一名受试者在给予400微克游离酸后出现中度腹泻外,未出现副作用。在第三组试验(n = 6)中,研究了80微克甲酯(抑制率为44±5%)和1.5毫克硫酸阿托品的联合作用。单独使用阿托品通过降低分泌量产生了43±6%的抑制作用。两者联合使用时抑制率为82±3%。胃内给予15(R)15 Me PGE2可剂量依赖性地抑制五肽胃泌素刺激的胃酸反应。该类似物的游离酸和甲酯之间的差异不显著。与其他Me PGE2化合物相比,15(R)15 Me PGE2每剂量的效果较差,但剂量范围更广且副作用轻微。同时给予阿托品具有显著的相加抑制作用。

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