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Research Article

Antisecretory Effect of Loperamide in Colon Epithelial Cells by Inhibition of Basolateral K+ Conductance

Pages 731-737 | Published online: 08 Jul 2009

References

  • Awouters F, Megens A, Verlinden M, Schuurkes J, Niemegeers C, Janssen PAJ. Loperamide. Survey of studies on mechanism of its antidiarrheal activity. Dig Dis Sci 1993;38:977–95.
  • Hughes S, Higgs NB, Turnberg LA. Loperamide has antisecretory activity in the human jejunum in vivo. Gut 1984;25:931–5.
  • Ahsan MA, Ilundain A, Naftalin RJ, Sandhu BK, Smith PM. Effects of theophylline, choleragen and loperamide on rabbit ileal fluid and electrolyte transport in vitro. Br J Pharmacol 1987;92:743–54.
  • Burleigh DE. Loperamide but not morphine has anti-secretory effects inhuman colon, in vitro. Eur J Pharmacol 1991;202:277–80.
  • Diener M, Knobloch SF, Rummel W. Action of loperamide on neuronally mediated and Ca+- and cAMP-mediated secretion in rat colon. Eur J Pharmacol 1988;152:217–25.
  • Kromer W. Unexpected prosecretory action of loperamide at μ-opioid receptors in the guinea-pig colonic mucosa in vitro. Br J Pharmacol 1995;114:739–44.
  • Piercey MF, Ruwart MJ. Naloxone inhibits the anti-diarrhoeal activity of loperamide. Br J Pharmacol 1979;66:373–5.
  • De Luca A, Coupar IM. Difenoxin and loperamide: studies on possible mechanisms of intestinal antisecretory action. Naunyn Schmiedebergs Arch Pharmacol 1993;347:231–7.
  • De Luca A, Coupar IM. Insights into opioid action in the intestinal tract. Pharmacol Ther 1996;69:103–15.
  • Merritt JE, Brown BL, Tomlinson S. Loperamide and calmodulin. Lancet 1982;1:283.
  • Zavecz JH, Jackson TE, Limp GL, Yellin TO. Relationship between anti-diarrhoeal activity and binding to calmodulin. Eur J Pharmacol 1982;78:375–7.
  • Kreusel KM, Fromm M, Schulzke JD, Hegel U. Cl-secretion in epithelial monolayers of mucus-forming human colon cells. Am J Physiol 1991;261:C574–82.
  • Epple HJ, Kreusel KM, Hanski C, Schulzke JD, Riecken EO, Fromm M. Differential stimulation of intestinal mucin secretion by cholera toxin and carbachol. Pflügers Arch 1997;433:638–47.
  • Fischer H, Illek B, Machen TE. Regulation of CFTR by protein phosphatase 2B and protein kinase C. Pfliigers Arch 1998;436: 175–81.
  • Schmitz H, Fromm M, Bentzel CJ, Scholz P, Detjen K, Mankertz J, et al. Tumor necrosis factor-alpha (TNFalpha) regulates the epithelial barrier in the human intestinal cell line HT-29/B6. J Cell Sci 1999;112:137–46.
  • Chang EB, Rao MC. Intestinal water and electrolyte transport: mechanism and physiological and adaptive processes. In: Johnson LR, editor. Physiology of the gastrointestinal tract. New York: Raven Press; 1994. p. 2027–81.
  • Vaandrager AB, Van den Berghe N, Bot AGM, De Jonge HR. Phorbol esters stimulate and inhibit Cl− secretion by different mechanisms in a colonic cell line. Am J Physiol 1992;262:G249–56.
  • Tai YH, Flick J, Levine SA, Madara JL, Sharp GW, Donowitz M. Regulation of tight junction resistance in T84 monolayers by elevation in intracellular Ca2+: a protein kinase C effect. J Membr Biol 1996;149:71–9.
  • Mandel K, McRoberts J, Beuerlein G, Foster E, Dharmsathap- horn K. Ba inhibition of VIP- and A23187-stimulated Cl secretion by T84 cell monolayers. Am J Physiol 1986;259: C486–94.
  • Mun EC, Mayol JM, Riegler M, O’Brien TC, Farokzhad OC, Song JC, et al. Levamisole inhibits intestinal Cl secretion via basolateral K+ channel blockade. Gastroenterology 1998;114:1257–67.
  • Sandle GI, Warhurst G, Butterfield I, Higgs NB, Lomax RB. Somatostatin inhibits basolateral potassium channels in human colonic crypts. Am J Physiol 1999;277:G967–75.
  • Sandhu BK, Tripp JH, Candy DCA, Harries JT. Loperamide: studies on its mechanism of action. Gut 1981;22:658–62.
  • Schulzke JD, Fromm M, Menge H, Reuter W, Riecken EO. Die neurogene Steuerung der Chlorid-Sekretion der Ileumschleim- haut. Z Gastroenterol 1986;24:62–9.
  • Gaginella TS, Rimele TJ, Wietecha M. Studies on rat intestinal epithelial cell receptors for serotonin and opiates. J Physiol-1983;335:101–11.
  • Lang ME, Davison JS, Bates SL, Meddings JB. Opioid receptors om guinea-pig intestinal crypt epithelial cells. J Physiol (Lond) 1996;497:161–74.
  • Nano JL, Fournel S, Rampal P. Characterization of δ-opioid receptors and effect of enkephalins on IRD 98 rat epithelial intestinal cell line. Pflügers Arch Eur J Physiol 2000;439: 547–54.
  • Rufo PA, Merlin D, Riegler M, Ferguson-Maltzmann MH, Dickinson BL, Brugnara C, et al. The antifungal antibiotic clotrimazole inhibits chloride secretion by human intestinal T84 cells via blockade of distinct basolateral K+ conductances. Demonstration of efficacy in intact rabbit colon and an in vivo mouse model of cholera. J Clin Invest 1997;100: 3111–20.
  • Tilly BC, Kansen M, van Gageldonk PG, van den Berghe N, Galjaard H, Bijman J, et al. G-proteins mediate intestinal chloride channel activation. J Biol Chem 1991;266:2036–40.
  • Prasad M, Smith JA, Resnick A, Awtrey CS, Hrnjez BJ, Matthews JB. Ammonia inhibits cAMP-regulated intestinal Cl− transport. Asymmetric effects of apical and basolateral exposure and implications for epithelial barrier function. J Clin Invest 1995;96:2142–51.
  • Lohrmann E, Burhoff I, Nitschke RB, Lang HJ, Mania D, Englert HC, et al. A new class of inhibitors of cAMP-mediated Cl− secretion in rabbit colon, acting by the reduction of cAMP- activated K+ conductance. Pflügers Arch 1995;429:517–30.
  • Niemegeers CJE, Lenaerts FM, Janssen PAJ. Loperamide (R 18553), a novel type of antidiarrheal agent. Part 1: In vivo oral pharmacology and acute toxicity. Comparison with morphine, codeine, diphenoxylate and difenoxine. Arzneim Forsch (Drug Res) 1974;24: 1633–6.
  • Heykants J, Michiels M, Knaeps A, Brugmans J. Loperamide (R 18553), a novel type of antidiarrheal agent. Part 5: The pharmacokinetics of loperamide in rats and man. Arzneim Forsch (Drug Res) 1974;24: 1649–53.
  • Leysen J, Laduron P. Aspecific binding, an important factor in drug action? J Pharmacol (Paris) 1977;8:565–6.
  • Wuster M, Herz A. Opiate agonist action of antidiarrheal agents in vitro and in vivo—findings in support of selective action. Naunyn Schmiedebergs Arch Pharmacol 1978;301:187–94.

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