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Chemical Compound Review

RIOPROSTIL     (2R,3S,4R)-4-hydroxy-2-(7- hydroxyheptyl)-3...

Synonyms: Rioprostilo, Rioprostilum, AC1NSKL0, SureCN186845, ORF-15927, ...
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Disease relevance of TR-4698


High impact information on TR-4698


Chemical compound and disease context of TR-4698


Biological context of TR-4698

  • Additional studies determined that administration of rioprostil at doses of 720, 1440, or 2160 micrograms/kg/24 hr (935-2805 times the gastroprotective ED50 in 24 hr pumps) was well tolerated, with only slight, transient increases in body temperature, softening of the stools, and mild sedation at the highest dose [13].
  • Pharmacokinetics of rioprostil in rats [14].
  • The effects of rioprostil on gastric emptying and intragastric acidity [15].
  • Thus, the metabolism of rioprostil proceeds via the biotransformation pathways of the naturally occurring prostaglandins [16].
  • The influence of rioprostil on the resting pressure of the lower oesophageal sphincter (LESP) and on the bolus-stimulated contraction wave amplitude of primary peristalsis is investigated in 9 healthy male volunteers receiving placebo or 300 micrograms and 600 micrograms of rioprostil orally in a randomized, double-blind, threefold crossover study [17].

Anatomical context of TR-4698


Associations of TR-4698 with other chemical compounds

  • This paper characterizes the ability of rioprostil, a synthetic primary alcohol prostaglandin E1 analog, to inhibit gastric acid secretion and prevent experimentally induced gastric lesions in rats and dogs, and determines the selectivity (the separation in potency) for these effects [18].
  • Misoprostol and rioprostil reduced integrated incremental responses of GIP by 57% (P less than or equal to 0.001) and 45% (P less than or equal to 0.01), respectively, and both gave rise to an initial (approximately 10 min) delay of insulin and C-peptide responses, without a significant overall reduction in integrated incremental responses [23].
  • In a double-blind crossover study, the gastric effects of a single oral dose of rioprostil (150 and 300 micrograms) or placebo were compared in basal conditions and during a 120-minute pentagastrin infusion [24].
  • A preliminary analysis on a group of 182 patients participating in a large, multicentre trial comparing nocturnal rioprostil, 600 micrograms and ranitidine, 300 mg, is presented [25].
  • In vitro experimental evidence suggests that the mechanism of the gastric antisecretory activity of rioprostil involves inhibition of the membrane bound histamine-stimulated adenylate cyclase [26].

Gene context of TR-4698

  • Rioprostil administration, 300 micrograms twice daily resulted in a significant decrease of fasting insulin, C-peptide, glucagon, and pancreatic polypeptide [27].
  • Basal serum gastrin levels and postprandial gastrin output are unchanged after treatment with rioprostil [28].
  • Rioprostil, given in a dose of 100 micrograms b.i.d. to rats for 1 week significantly increases antral mucosal height but has no influence on the mucosal concentrations and cell densities of the gastric peptides, gastrin and somatostatin [28].
  • The integrated 3-hour plasma gastrin response to the peptone meals was not significantly changed by any of the doses of rioprostil [29].
  • In addition, in these rats rioprostil increased mucin levels and did not cause dermal irritation [30].

Analytical, diagnostic and therapeutic context of TR-4698


  1. Rioprostil and duodenal ulcer. Howden, C.W. Lancet (1986) [Pubmed]
  2. Rioprostil heals pre-existing aspirin-induced gastric lesions in dogs during daily aspirin administration without altering the anti-inflammatory or analgesic efficacy of aspirin. Katz, L.B., Shriver, D.A. J. Pharmacol. Exp. Ther. (1989) [Pubmed]
  3. Antiulcer effect of rioprostil, a prostaglandin E1 analog, in combination with antacid. Katz, L.B., Genna, T., Shriver, D.A. Life Sci. (1986) [Pubmed]
  4. Cytoprotective and dose-dependent inhibitory effects of prostaglandin E1 on rat pancreas treated with ciclosporin A. Müller, M.K., Wojzek, M., Rünzi, M., von Schönfeld, J., Goebell, H., Singer, M.V. Digestion (1991) [Pubmed]
  5. Antisecretory and antigastrin effects of rioprostil in gastric fistula dogs. Katz, L.B., Genna, T., Greeley, G.H., Shriver, D.A. Dig. Dis. Sci. (1987) [Pubmed]
  6. Night-time rioprostil versus ranitidine in duodenal ulcer healing. Dammann, H.G., Walter, T.A., Müller, P., Simon, B. Lancet (1986) [Pubmed]
  7. Prevention of toxic effects of cyclosporin on pancreatic B-cells of rats by Rioprostil, a new prostaglandin analogue. Müller, M.K., Degenhardt, H., Klöppel, G., Goebell, H., Bergmann, K., Löhr, M. Gut (1988) [Pubmed]
  8. The interaction of the prostaglandin E derivative rioprostil with oral anticoagulant agents. Thijssen, H.H., Hamulyàk, K. Clin. Pharmacol. Ther. (1989) [Pubmed]
  9. Rioprostil: a clinical experience in gastric ulcer treatment. Mascio, G., Guida, L., Mascio, M.V., Maggiolo, F. International journal of clinical pharmacology research. (1988) [Pubmed]
  10. Prostaglandin analogue protects pancreatic B-cells against cyclosporin A toxicity. Löhr, M., Müller, M.K., Goebell, H., Klöppel, G. Experientia (1989) [Pubmed]
  11. Rioprostil in the short-term treatment of duodenal ulcer: a multicentre double-blind trial vs. cimetidine. Bianchi Porro, G., Parente, F., Hentschel, E., Bennani, A., Sebti, F., Cherkaoui, A., Demyttenaere, M., Gouerou, H., Blasi, A., Darnis, F. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  12. Prostaglandins in clinical treatment of gastroduodenal mucosal lesions: a review. Aly, A. Scand. J. Gastroenterol. Suppl. (1987) [Pubmed]
  13. Slow release delivery of rioprostil by an osmotic pump inhibits the formation of acute aspirin-induced gastric lesions in dogs and accelerates the healing of chronic lesions without incidence of side effects. Katz, L.B., Shriver, D.A. Toxicol. Appl. Pharmacol. (1989) [Pubmed]
  14. Pharmacokinetics of rioprostil in rats. Petersen-von Gehr, J.K., Siefert, H.M., Steinke, W. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  15. The effects of rioprostil on gastric emptying and intragastric acidity. Penston, J.G., Johnston, D.A., Wormsley, K.G. Hepatogastroenterology (1986) [Pubmed]
  16. Metabolic fate of rioprostil in the rat--in vivo and in liver perfusion. Ahr, H.J., Karl, W., Scherling, D., Wünsche, C. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  17. Effect of rioprostil, an oral prostaglandin E1 analogue, on lower oesophageal sphincter pressure and on the motility of the distal oesophagus in healthy volunteers. Baunack, A.R., Demol, P., Froese, G., Kuhlmann, J., Weihrauch, T.R. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  18. Selective gastric antilesion properties of rioprostil, a prostaglandin E1 analog, in rats and dogs. Katz, L.B., Shriver, D.A., Tobia, A.J., Rosenthale, M.E. J. Pharmacol. Exp. Ther. (1987) [Pubmed]
  19. Effect of rioprostil and colchicine on CCl4-acute liver damage in rats. Relationship with plasma membrane lipids. Mourelle, M., Amezcua, J.L., Hong, E. Prostaglandins (1987) [Pubmed]
  20. Rioprostil, a new prostaglandin E1, prevents cyclosporin A-induced damage to endocrine and exocrine pancreas. Müller, M., Degenhardt, H., Bergmann, K., Coone, H., Löhr, M., Klöppel, G., Goebell, H. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  21. Protective effect of rioprostil on indomethacin-induced lesions of gastric and duodenal mucosa in healthy volunteers. Vlahov, V., Kirkov, V., Popov, P., Gerova, Z. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  22. Effect of rioprostil on the gastric acid and bicarbonate secretion in patients with gastric ulcer. Krastev, Z., Deredjian, S., Matincheva, R., Spasova, Z., Karakasheva, V. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  23. Effects of four orally administered analogues of prostaglandin E1 and E2 on glucose tolerance and on the secretion of pancreatic and gastrointestinal hormones in man. Nauck, M., Härter, S., Ebert, R., Creutzfeldt, W. Eur. J. Clin. Invest. (1989) [Pubmed]
  24. Gastric effects of a prostaglandin E1-derivate (rioprostil) on acid, alkaline, and mucus secretion. Guslandi, M., Passaretti, S., Tittobello, A., Fasani, R. Clinical therapeutics. (1986) [Pubmed]
  25. Rioprostil in the healing of duodenal ulceration: a short report. Whorwell, P.J. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  26. Gastric antisecretory and antigastrolesive pharmacology of rioprostil. Shriver, D.A., Katz, L.B., Rosenthale, M.E. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  27. Effect of rioprostil, a methylprostaglandin E1 analog, on basal and stimulated plasma pancreatic hormone levels in man. Segers, O., Somers, G. Dig. Dis. Sci. (1990) [Pubmed]
  28. Influence of chronic rioprostil treatment on gastric endocrine function. Koop, H., Schwarting, H., Eckel, U., Wagenknecht, J., Hallfeldt, U., Arnold, R. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
  29. Effect of rioprostil, a synthetic prostaglandin E1 on meal-stimulated gastric acid secretion and plasma gastrin levels in humans. Schulte, K., Singer, M.V., Eysselein, V., Demol, P., Goebell, H. Digestion (1987) [Pubmed]
  30. Antigastrolesive, gastric antisecretory, diarrheagenic and mucus-stimulating effects in rats following topically applied rioprostil, a synthetic prostaglandin E1 analog. Katz, L.B., Genna, T., Scott, C.K., Rosenthale, M.E., Shriver, D.A. Life Sci. (1987) [Pubmed]
  31. Preventive and curative effects of prostaglandins on stress ulcer in rats. Application of endoscopic observation. Yoshimura, H., Kan, N., Ogawa, N. Dig. Dis. Sci. (1989) [Pubmed]
  32. Treatment of duodenal ulcer with rioprostil: a randomized multicentre double-blind study. Boucekkine, T., Meknini, B., Bitoun, A., Prunièras, F., Khedis, A., de Lauture, D., Rotenberg, A., Molinie, C., Roux, M., Gauthier, A. Scand. J. Gastroenterol. Suppl. (1989) [Pubmed]
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