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前列腺素E1诱导的人空肠分泌:剂量反应研究。

Human jejunal secretion induced by prostaglandin E1: a dose-response study.

作者信息

Sobhani I, Vidon N, Huchet B, Rambaud J C

机构信息

INSERM U. 290, Hôpital Saint Lazare, Paris, France.

出版信息

Br J Clin Pharmacol. 1991 Apr;31(4):433-7. doi: 10.1111/j.1365-2125.1991.tb05559.x.

Abstract
  1. Intraluminally infused prostaglandins induce jejunal secretion of water and electrolytes in man, and a receptor-mediated process in the intestinal epithelial cells has been suggested to explain this secretion. In an attempt to obtain data under basal conditions for pharmacological studies, we tested the dose-response effect of PGE1 on jejunal hydroelectrolytic movements in 10 healthy volunteers. 2. Accordingly, a solution with or without PGE1 was infused via a four-lumen tube with a proximal occluding balloon and jejunal water and electrolyte transport were determined. The segment tested was 40 cm long. Seven randomized doses of PGE1 ranging from 0.01 to 1.3 micrograms kg-1 min-1 (2.83 to 364 pmol kg-1 min-1) were infused in an isotonic control saline solution. The secretion induced by PGE1 was evaluated in each subject as the difference between fluxes in response to the control saline solution and to PGE1. 3. Whatever the dose, PGE1 induced secretion of water, Na+, K+ and Cl- which was dose-dependent and saturable, with a mean Km of congruent to 6-8 pmol kg-1 min-1, suggesting that at the pharmacological doses used, enterocytes have a saturable membrane site similar to a single class of receptor for PGE1. 4. These findings may be of great importance if prostaglandins are administered as drugs or used as jejunal secretory agents in vivo when the antisecretory effect of another drug is studied.
摘要
  1. 腔内注入前列腺素可诱导人体空肠分泌水和电解质,有人提出肠上皮细胞中的受体介导过程可解释这种分泌。为了获取基础条件下的数据用于药理学研究,我们检测了10名健康志愿者中前列腺素E1(PGE1)对空肠水电解质运动的剂量反应效应。2. 因此,通过带有近端阻塞球囊的四腔管注入含或不含PGE1的溶液,并测定空肠水和电解质转运。检测的肠段长40厘米。在等渗对照盐溶液中注入7种随机剂量的PGE1,范围为0.01至1.3微克/千克·分钟(2.83至364皮摩尔/千克·分钟)。PGE1诱导的分泌在每个受试者中通过对照盐溶液和PGE1反应通量之间的差异来评估。3. 无论剂量如何,PGE1均可诱导水、钠、钾和氯的分泌,其呈剂量依赖性且可饱和,平均米氏常数约为6 - 8皮摩尔/千克·分钟,这表明在所使用的药理学剂量下,肠上皮细胞具有类似于单一类PGE1受体的可饱和膜位点。4. 如果在研究另一种药物的抗分泌作用时将前列腺素作为药物给药或用作体内空肠分泌剂,这些发现可能具有重要意义。

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Lanreotide inhibits human jejunal secretion induced by prostaglandin E1 in healthy volunteers.
Br J Clin Pharmacol. 1996 Feb;41(2):109-14. doi: 10.1111/j.1365-2125.1996.tb00167.x.

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Prostaglandin E2-binding sites and cAMP production in porcine fundic mucosa.
Am J Physiol. 1981 Oct;241(4):G313-20. doi: 10.1152/ajpgi.1981.241.4.G313.

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