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Chemical Compound Review

AC1NUPCX     1-[[(E)-[5- (hydroxymethyl)indol-3...

Synonyms: SureCN16465, HTF 919, SDZ HTF-919, DCL001044, DNC000745, ...
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Disease relevance of Zelmac

  • Tegaserod accelerates orocecal transit in patients with constipation-predominant irritable bowel syndrome [1].
  • Novel approaches include alosetron; a 5-HT(3) antagonist, tegaserod, a partial 5-HT(4) agonist, kappa-opioid agonists, and neurokinin antagonists to address the remaining challenging symptoms of pain, constipation, and bloating [2].
  • Reductions in the number of days with at least moderate abdominal pain/discomfort, bloating, no bowel movements, and hard/lumpy stools were greater in the tegaserod group compared with the placebo group [3].
  • On the basis of tegaserod's mechanism of action, it was hypothesized that tegaserod may accelerate the return of gastric function in intensive care unit patients with gastroparesis [4].
  • The use of tegaserod in critically ill patients with impaired gastric motility [4].

Psychiatry related information on Zelmac

  • Effect of tegaserod on esophageal pain threshold, regurgitation, and symptom relief in patients with functional heartburn and mechanical sensitivity [5].
  • It would also be of interest to know whether treatment with tegaserod leads either directly, or indirectly, to changes in visceral sensitivity or psychopathology, which are also considered important in the pathophysiology of this condition [6].

High impact information on Zelmac


Chemical compound and disease context of Zelmac


Biological context of Zelmac


Anatomical context of Zelmac

  • Tegaserod can act as a promotile agent throughout the gastrointestinal tract [18].
  • Therefore, this study aimed to evaluate the effects of tegaserod on gallbladder contractility and on functional status of the sphincter of Oddi during both the interdigestive and the digestive periods in healthy female subjects and in female patients with IBS-C [17].
  • Tegaserod shortened the small intestine transit time by 30% after oral and by 37% after intravenous administration [18].
  • Exposure of rat colonic mucosa to tegaserod in the range of 5 nM to 5 muM for 5 or 10 min caused rapid time- and concentration-dependent desensitization of the peristaltic reflex induced by mucosal stroking, consistent with the operation of a rapidly desensitizing 5-HT(4b) receptor subtype [19].
  • Tegaserod does not alter fasting or meal-induced biliary tract motility [17].

Associations of Zelmac with other chemical compounds


Gene context of Zelmac


Analytical, diagnostic and therapeutic context of Zelmac


  1. Tegaserod accelerates orocecal transit in patients with constipation-predominant irritable bowel syndrome. Prather, C.M., Camilleri, M., Zinsmeister, A.R., McKinzie, S., Thomforde, G. Gastroenterology (2000) [Pubmed]
  2. Management of the irritable bowel syndrome. Camilleri, M. Gastroenterology (2001) [Pubmed]
  3. An Asia-Pacific, double blind, placebo controlled, randomised study to evaluate the efficacy, safety, and tolerability of tegaserod in patients with irritable bowel syndrome. Kellow, J., Lee, O.Y., Chang, F.Y., Thongsawat, S., Mazlam, M.Z., Yuen, H., Gwee, K.A., Bak, Y.T., Jones, J., Wagner, A. Gut (2003) [Pubmed]
  4. The use of tegaserod in critically ill patients with impaired gastric motility. Banh, H.L., MacLean, C., Topp, T., Hall, R. Clin. Pharmacol. Ther. (2005) [Pubmed]
  5. Effect of tegaserod on esophageal pain threshold, regurgitation, and symptom relief in patients with functional heartburn and mechanical sensitivity. Rodriguez-Stanley, S., Zubaidi, S., Proskin, H.M., Kralstein, J.R., Shetzline, M.A., Miner, P.B. Clinical gastroenterology and hepatology : the official clinical practice journal of the American Gastroenterological Association. (2006) [Pubmed]
  6. Tegaserod for the treatment of irritable bowel syndrome. Evans, B.W., Clark, W.K., Moore, D.J., Whorwell, P.J. Cochrane database of systematic reviews (Online) (2004) [Pubmed]
  7. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gershon, M.D., Tack, J. Gastroenterology (2007) [Pubmed]
  8. Clinical pharmacokinetics of tegaserod, a serotonin 5-HT(4) receptor partial agonist with promotile activity. Appel-Dingemanse, S. Clinical pharmacokinetics. (2002) [Pubmed]
  9. The effects of tegaserod (HTF 919) on oesophageal acid exposure in gastro-oesophageal reflux disease. Kahrilas, P.J., Quigley, E.M., Castell, D.O., Spechler, S.J. Aliment. Pharmacol. Ther. (2000) [Pubmed]
  10. Subject's Global Assessment of Relief: an appropriate method to assess the impact of treatment on irritable bowel syndrome-related symptoms in clinical trials. Müller-Lissner, S., Koch, G., Talley, N.J., Drossman, D., Rueegg, P., Dunger-Baldauf, C., Lefkowitz, M. Journal of clinical epidemiology. (2003) [Pubmed]
  11. The effects of tegaserod (HTF 919) on the pharmacokinetics and pharmacodynamics of digoxin in healthy subjects. Zhou, H., Horowitz, A., Ledford, P.C., Hubert, M., Appel-Dingemanse, S., Osborne, S., McLeod, J.F. Journal of clinical pharmacology. (2001) [Pubmed]
  12. Tegaserod for constipation-predominant irritable bowel syndrome. Kale-Pradhan, P.B., Wilhelm, S.M. Pharmacotherapy (2007) [Pubmed]
  13. Review: good evidence supports polyethylene glycol and tegaserod for constipation. Andrews, C.N., Bharucha, A.E. ACP J. Club (2005) [Pubmed]
  14. Tegaserod. Scott, L.J., Perry, C.M. Drugs (1999) [Pubmed]
  15. The 5-HT4 receptor agonist, tegaserod, is a potent 5-HT2B receptor antagonist in vitro and in vivo. Beattie, D.T., Smith, J.A., Marquess, D., Vickery, R.G., Armstrong, S.R., Pulido-Rios, T., McCullough, J.L., Sandlund, C., Richardson, C., Mai, N., Humphrey, P.P. Br. J. Pharmacol. (2004) [Pubmed]
  16. Long-term safety of tegaserod in patients with constipation-predominant irritable bowel syndrome. Tougas, G., Snape, W.J., Otten, M.H., Earnest, D.L., Langaker, K.E., Pruitt, R.E., Pecher, E., Nault, B., Rojavin, M.A. Aliment. Pharmacol. Ther. (2002) [Pubmed]
  17. Tegaserod does not alter fasting or meal-induced biliary tract motility. Fisher, R.S., Thistle, J., Lembo, A., Novick, J., O'Kane, P., Chey, W.D., Beglinger, C., Rueegg, P., Shi, V., Dogra, A., Luo, D., Earnest, D.L. Am. J. Gastroenterol. (2004) [Pubmed]
  18. Tegaserod, a 5-HT4 receptor partial agonist, accelerates gastric emptying and gastrointestinal transit in healthy male subjects. Degen, L., Matzinger, D., Merz, M., Appel-Dingemanse, S., Osborne, S., Lüchinger, S., Bertold, R., Maecke, H., Beglinger, C. Aliment. Pharmacol. Ther. (2001) [Pubmed]
  19. Desensitization of the peristaltic reflex induced by mucosal stimulation with the selective 5-HT4 agonist tegaserod. Grider, J.R. Am. J. Physiol. Gastrointest. Liver Physiol. (2006) [Pubmed]
  20. Omeprazole delays gastric emptying in healthy volunteers: an effect prevented by tegaserod. Tougas, G., Earnest, D.L., Chen, Y., Vanderkoy, C., Rojavin, M. Aliment. Pharmacol. Ther. (2005) [Pubmed]
  21. Modulation of intestinal gas dynamics in healthy human volunteers by the 5-HT receptor agonist tegaserod. Coleski, R., Owyang, C., Hasler, W.L. Am. J. Gastroenterol. (2006) [Pubmed]
  22. Effects of tegaserod on Fos, substance P and calcitonin gene-related peptide expression induced by colon inflammation in lumbarsacral spinal cord. Sun, Y.N., Luo, J.Y. World J. Gastroenterol. (2004) [Pubmed]
  23. Noninvasive assessment of gastric emptying by near-infrared fluorescence reflectance imaging in mice: pharmacological validation with tegaserod, cisapride, and clonidine. Gremlich, H.U., Martínez, V., Kneuer, R., Kinzy, W., Weber, E., Pfannkuche, H.J., Rudin, M. Molecular imaging : official journal of the Society for Molecular Imaging. (2004) [Pubmed]
  24. In vitro metabolism of tegaserod in human liver and intestine: assessment of drug interactions. Vickers, A.E., Zollinger, M., Dannecker, R., Tynes, R., Heitz, F., Fischer, V. Drug Metab. Dispos. (2001) [Pubmed]
  25. Regional gastric contractility alterations in a diabetic gastroparesis mouse model: effects of cholinergic and serotoninergic stimulation. James, A.N., Ryan, J.P., Crowell, M.D., Parkman, H.P. Am. J. Physiol. Gastrointest. Liver Physiol. (2004) [Pubmed]
  26. Tegaserod inhibits noxious rectal distention induced responses and limbic system c-Fos expression in rats with visceral hypersensitivity. Jiao, H.M., Xie, P.Y. World J. Gastroenterol. (2004) [Pubmed]
  27. Tegaserod: a review of its use in the management of irritable bowel syndrome with constipation in women. Wagstaff, A.J., Frampton, J.E., Croom, K.F. Drugs (2003) [Pubmed]
  28. Systematic review: incidence of abdominal/pelvic surgery amongst patients using tegaserod in randomized controlled trials. Schoenfeld, P. Aliment. Pharmacol. Ther. (2004) [Pubmed]
  29. Tegaserod is effective in the initial and retreatment of irritable bowel syndrome with constipation. Müller-Lissner, S., Holtmann, G., Rueegg, P., Weidinger, G., Löffler, H. Aliment. Pharmacol. Ther. (2005) [Pubmed]
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