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Human jejunal secretion induced by prostaglandin E1: a dose-response study
Authors:I Sobhani  N Vidon  B Huchet  J C Rambaud
Affiliation:INSERM U. 290, Hôpital Saint Lazare, Paris, France.
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.
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[2]、R E Garris,C F Kirkwood.Misoprostol: a prostaglandin E1 analogue[J].Clinical pharmacy,1989,8(9):627-644.
[3]、P Demol,W Wingender,T R Weihrauch,K H Graefe.Inhibition of gastric secretion in man by rioprostil, a new synthetic methyl prostaglandin E1[J].Arzneimittel-Forschung,1985,35(5):861-863.
[4]、K Takeuchi,H Niida,Y Takinami,S Okabe.Stimulation by prostaglandin E2 of alkaline secretion in the rat duodenum: comparative study with hypertonic NaCl[J].Japanese journal of pharmacology,1990,53(1):67-74.
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[6]、R L McIsaac,B J Johnston,M C Flannery,L P Fielding.Gastric acid secretion induced by impromidine in the dog and man: analysis of dose-response relationships[J].Agents and actions,1982,12(1-2):166-167.
[7]、Samuelsson B,Morgenstern R,Jakobsson PJ.Membrane prostaglandin E synthase-1: a novel therapeutic target[J].Pharmacological reviews,2007,59(3):207-224.
[8]、J K Ramage,A Denton,J G Williams.Inhibition of food stimulated acid secretion by misoprostol, an orally active synthetic E1 analogue prostaglandin[J].British journal of clinical pharmacology,1985,19(1):9-12.
[9]、A. G. Press,K. Ewe,J. Schmidt,H. Junge.Effect of loperamide on jejunal electrolyte and water transport,prostaglandin E 2-induced secretion and intestinal transit time in man[J].European journal of clinical pharmacology,1991,41(3):239-243.
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[11]、J. A. Brock and,T. C. Cunnane.Inhibition of purinergic transmission by prostaglandin E1 and E2 in the guinea-pig vas deferens: an electrophysiological study.[J].British journal of pharmacology,1996,118(3):776-782.
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[13]、P Rafferty, J G Varley, J S Edwards, and,S T Holgate.Inhibition of exercise-induced asthma by nifedipine: a dose-response study.[J].British journal of clinical pharmacology,1987,24(4):479-484.
[14]、Wen-tong FANG Hong-jian LI Liao-sheng ZHOU.Protective effects of prostaglandin E1 on human umbilical vein endothelial cell injury induced by hydrogen peroxide[J].Acta pharmacologica Sinica,2010,31(4):485-492.
[15]、D Giugliano,R Torella,F D\'Onofrio.Arguments for an inhibiting role of prostaglandin E1 on insulin secretion in man.[J].Il Farmaco; edizione scientifica,1979,34(2):157-164.
[16]、Y. Mizushima,K. Hoshi,H. Aihara,M. Kurachi.Inhibition of bronchoconstriction by aerosol of a lipid emulsion containing prostaglandin E1[J].The Journal of pharmacy and pharmacology,1983,35(6):397-397.
[17]、G. Thomas,P. V. V. Prasada Rao.Leucocyte migration and prostaglandin E1[J].The Journal of pharmacy and pharmacology,1979,31(1):789-791.
[18]、Huang DY,Richter K,Breidenbach A,Vallon V.Human C-peptide acutely lowers glomerular hyperfiltration and proteinuria in diabetic rats: a dose-response study[J].Naunyn-Schmiedeberg\'s archives of pharmacology,2002,365(1):67-73.
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[20]、J R Hoyland,L B Kier.Preferred conformation of prostaglandin E 1[J].Journal of medicinal chemistry,1972,15(1):84-86.
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