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Chemical Compound Review

Zofran     9-methyl-3-[(2- methylimidazol-1- yl)methyl]...

Synonyms: Zophren, Zuplenz, Zudan, ondansetron, CHEMBL46, ...
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Disease relevance of Zofran


Psychiatry related information on Zofran


High impact information on Zofran


Chemical compound and disease context of Zofran


Biological context of Zofran


Anatomical context of Zofran

  • The following inhibition was fully antagonized by ketotifen (mast cell stabilizer), granisetron and ondansetron (5-HT3 antagonists), RP-67,580 (NK1 antagonist), and perivagal capsaicin pretreatment [24].
  • METHODS: The effects of ondansetron and placebo on fasting and postprandial colonic tone and motility in 10 patients with carcinoid diarrhea were compared using a manometry-barostat assembly positioned in the upper descending colon [25].
  • METHODS: Twenty patients who received 4 days of TBI as part of their preparative regimen before bone marrow transplantation were randomized to receive either 8-mg oral doses of ondansetron or placebo [19].
  • The effects of ondansetron, a potent and selective antagonist of the 5-HT3 receptor, were examined on (1) frequency of the hippocampal theta rhythm, (2) induction of LTP in field CA1 of freely moving rats, and (3) retention of olfactory and spatial memory in tasks known to depend on an intact hippocampus [26].
  • The pA2 of some selected compounds against the 5-HT3 agonist 2-methyl-5HT in the guinea pig ileum was in the range of tropisetron or ondansetron, and one of them, 7e, was more potent than these reference compounds by approximately 2 or 3 orders of magnitude [27].

Associations of Zofran with other chemical compounds

  • The results suggest that the suppression of gastric activity fronts is achieved via the suppression of plasma motilin peaks because in the presence of ondansetron a motilin agonist like erythromycin restores the gastric phase 3 [6].
  • CONCLUSION: Oral ondansetron is a safe and effective antiemetic that is more efficacious than placebo for patients receiving cyclophosphamide-based chemotherapy [14].
  • PATIENTS AND METHODS: Cancer patients (n = 609) receiving first-course cisplatin chemotherapy were randomized to one of three treatments: 1.8 or 2.4 mg/kg dolasetron mesylate salt (equivalent to 1.3 and 1.8 mg/kg dolasetron base, respectively) or 32 mg ondansetron [28].
  • This study sought to investigate whether efficacy of antiemetic treatment with ondansetron and tropisetron depends on cytochrome P-450 2D6 (CYP2D6) genotype, hypothesizing that the rapid and particularly the ultrarapid metabolizers of these drugs are at risk of being undertreated [17].
  • CONCLUSION: Metopimazine plus ondansetron was significantly superior to ondansetron alone, concerning all efficacy parameters assessed, in patients who received platinum-based chemotherapy [29].

Gene context of Zofran

  • Ondansetron chronic effect on CCK-4-induced behavioral changes needs further exploration [30].
  • Docking of 5-HT3 antagonists granisetron, tropisetron, ondansetron, dolasetron ('setrons), and (+)-tubocurarine suggests an aromatic binding cleft behind a hydrophilic vestibule [31].
  • To determine if this pathway plays a role in the pathophysiology of inflammation, we investigated the effects of spinally administered ondansetron (a selective 5HT3 receptor antagonist) on deep dorsal horn neuronal responses in carrageenan inflamed and naïve animals using in vivo electrophysiology [32].
  • We offer several alternative explanations for this event, all of which rest on disruption of serotonergic and/or dopaminergic transmission and which could also involve inhibition by paroxetine of the P450 enzyme, CYP2D6, which metabolizes ondansetron [33].
  • To summarize, this study has identified the involvement of CYP2D6 in the formation of the hydroxylated metabolites of tropisetron and ondansetron and in addition of CYP3A in ondansetron hydroxylation [34].

Analytical, diagnostic and therapeutic context of Zofran


  1. Comparison of the 5-hydroxytryptamine3 (serotonin) antagonist ondansetron (GR 38032F) with high-dose metoclopramide in the control of cisplatin-induced emesis. Marty, M., Pouillart, P., Scholl, S., Droz, J.P., Azab, M., Brion, N., Pujade-Lauraine, E., Paule, B., Paes, D., Bons, J. N. Engl. J. Med. (1990) [Pubmed]
  2. Ondansetron for pruritus due to cholestasis. Raderer, M., Müller, C., Scheithauer, W. N. Engl. J. Med. (1994) [Pubmed]
  3. Improvement of cholestatic pruritus by ondansetron. Schwörer, H., Ramadori, G. Lancet (1993) [Pubmed]
  4. Effect of decreasing afferent vagal activity with ondansetron on symptoms of bulimia nervosa: a randomised, double-blind trial. Faris, P.L., Kim, S.W., Meller, W.H., Goodale, R.L., Oakman, S.A., Hofbauer, R.D., Marshall, A.M., Daughters, R.S., Banerjee-Stevens, D., Eckert, E.D., Hartman, B.K. Lancet (2000) [Pubmed]
  5. Ondansetron and hyperemesis gravidarum. World, M.J. Lancet (1993) [Pubmed]
  6. 5-hydroxytryptamine-3 receptors are involved in the initiation of gastric phase-3 motor activity in humans. Wilmer, A., Tack, J., Coremans, G., Janssens, J., Peeters, T., Vantrappen, G. Gastroenterology (1993) [Pubmed]
  7. A single-blind comparison of intravenous ondansetron, a selective serotonin antagonist, with intravenous metoclopramide in the prevention of nausea and vomiting associated with high-dose cisplatin chemotherapy. Hainsworth, J., Harvey, W., Pendergrass, K., Kasimis, B., Oblon, D., Monaghan, G., Gandara, D., Hesketh, P., Khojasteh, A., Harker, G. J. Clin. Oncol. (1991) [Pubmed]
  8. Ondansetron alters human alcohol intoxication. Swift, R.M., Davidson, D., Whelihan, W., Kuznetsov, O. Biol. Psychiatry (1996) [Pubmed]
  9. Ondansetron treatment in Tourette's disorder: a 3-week, randomized, double-blind, placebo-controlled study. Toren, P., Weizman, A., Ratner, S., Cohen, D., Laor, N. The Journal of clinical psychiatry. (2005) [Pubmed]
  10. Ondansetron plus metopimazine compared with ondansetron alone in patients receiving moderately emetogenic chemotherapy. Herrstedt, J., Sigsgaard, T., Boesgaard, M., Jensen, T.P., Dombernowsky, P. N. Engl. J. Med. (1993) [Pubmed]
  11. Efficacy of ondansetron (GR 38032F) and the role of serotonin in cisplatin-induced nausea and vomiting. Cubeddu, L.X., Hoffmann, I.S., Fuenmayor, N.T., Finn, A.L. N. Engl. J. Med. (1990) [Pubmed]
  12. Pancreatitis associated with ondansetron. Alberti-Flor, J.J. J. Natl. Cancer Inst. (1995) [Pubmed]
  13. The serotonin signaling system: from basic understanding to drug development for functional GI disorders. Gershon, M.D., Tack, J. Gastroenterology (2007) [Pubmed]
  14. Efficacy of oral ondansetron in the prevention of emesis in outpatients receiving cyclophosphamide-based chemotherapy. The Ondansetron Study Group. Beck, T.M., Ciociola, A.A., Jones, S.E., Harvey, W.H., Tchekmedyian, N.S., Chang, A., Galvin, D., Hart, N.E. Ann. Intern. Med. (1993) [Pubmed]
  15. Single-dose oral granisetron has equivalent antiemetic efficacy to intravenous ondansetron for highly emetogenic cisplatin-based chemotherapy. Gralla, R.J., Navari, R.M., Hesketh, P.J., Popovic, W., Strupp, J., Noy, J., Einhorn, L., Ettinger, D., Bushnell, W., Friedman, C. J. Clin. Oncol. (1998) [Pubmed]
  16. Is oral ondansetron really efficacious in the control of cisplatin-induced delayed emesis? Martin, M. J. Clin. Oncol. (1996) [Pubmed]
  17. Patient-tailored antiemetic treatment with 5-hydroxytryptamine type 3 receptor antagonists according to cytochrome P-450 2D6 genotypes. Kaiser, R., Sezer, O., Papies, A., Bauer, S., Schelenz, C., Tremblay, P.B., Possinger, K., Roots, I., Brockmöller, J. J. Clin. Oncol. (2002) [Pubmed]
  18. Prevention of cyclophosphamide/cytarabine-induced emesis with ondansetron in children with leukemia. Carden, P.A., Mitchell, S.L., Waters, K.D., Tiedemann, K., Ekert, H. J. Clin. Oncol. (1990) [Pubmed]
  19. Randomized double-blind, placebo-controlled evaluation of oral ondansetron in the prevention of nausea and vomiting associated with fractionated total-body irradiation. Spitzer, T.R., Bryson, J.C., Cirenza, E., Foelber, R., Wallerstadt, M., Stout, C., Kunka, R.L., Plagge, P.B., Dubois, A. J. Clin. Oncol. (1994) [Pubmed]
  20. Improved p50 auditory gating with ondansetron in medicated schizophrenia patients. Adler, L.E., Cawthra, E.M., Donovan, K.A., Harris, J.G., Nagamoto, H.T., Olincy, A., Waldo, M.C. The American journal of psychiatry. (2005) [Pubmed]
  21. Pharmacokinetics of intravenous ondansetron in healthy children undergoing ear, nose, and throat surgery. Spahr-Schopfer, I.A., Lerman, J., Sikich, N., Palmer, J., Jorch, U. Clin. Pharmacol. Ther. (1995) [Pubmed]
  22. The effect of rifampin on the pharmacokinetics of oral and intravenous ondansetron. Villikka, K., Kivistö, K.T., Neuvonen, P.J. Clin. Pharmacol. Ther. (1999) [Pubmed]
  23. Effect of acupuncture compared with placebo-acupuncture at P6 as additional antiemetic prophylaxis in high-dose chemotherapy and autologous peripheral blood stem cell transplantation: a randomized controlled single-blind trial. Streitberger, K., Friedrich-Rust, M., Bardenheuer, H., Unnebrink, K., Windeler, J., Goldschmidt, H., Egerer, G. Clin. Cancer Res. (2003) [Pubmed]
  24. Role of 5-HT3 receptors and afferent fibers in the effects of mast cell degranulation on colonic motility in rats. Castex, N., Fioramonti, J., Fargeas, M.J., More, J., Bueno, L. Gastroenterology (1994) [Pubmed]
  25. A 5HT3 antagonist corrects the postprandial colonic hypertonic response in carcinoid diarrhea. von der Ohe, M.R., Camilleri, M., Kvols, L.K. Gastroenterology (1994) [Pubmed]
  26. Effects of 5-HT3 receptor antagonism on hippocampal theta rhythm, memory, and LTP induction in the freely moving rat. Stäubli, U., Xu, F.B. J. Neurosci. (1995) [Pubmed]
  27. Novel antagonists of 5-HT3 receptors. Synthesis and biological evaluation of piperazinylquinoxaline derivatives. Monge, A., Palop, J.A., Del Castillo, J.C., Calderó, J.M., Roca, J., Romero, G., Del Río, J., Lasheras, B. J. Med. Chem. (1993) [Pubmed]
  28. Double-blind, randomized comparison of the antiemetic efficacy of intravenous dolasetron mesylate and intravenous ondansetron in the prevention of acute cisplatin-induced emesis in patients with cancer. Dolasetron Comparative Chemotherapy-induced Emesis Prevention Group. Hesketh, P., Navari, R., Grote, T., Gralla, R., Hainsworth, J., Kris, M., Anthony, L., Khojasteh, A., Tapazoglou, E., Benedict, C., Hahne, W. J. Clin. Oncol. (1996) [Pubmed]
  29. Randomized, double-blind comparison of ondansetron versus ondansetron plus metopimazine as antiemetic prophylaxis during platinum-based chemotherapy in patients with cancer. Herrstedt, J., Sigsgaard, T., Handberg, J., Schousboe, B.M., Hansen, M., Dombernowsky, P. J. Clin. Oncol. (1997) [Pubmed]
  30. Acute and chronic role of 5-HT3 neuronal system on behavioral and neuroendocrine changes induced by intravenous cholecystokinin tetrapeptide administration in humans. Dépôt, M., Caillé, G., Mukherjee, J., Katzman, M.A., Cadieux, A., Bradwejn, J. Neuropsychopharmacology (1999) [Pubmed]
  31. Binding interactions of antagonists with 5-hydroxytryptamine3A receptor models. Maksay, G., Bikádi, Z., Simonyi, M. J. Recept. Signal Transduct. Res. (2003) [Pubmed]
  32. Descending serotonergic facilitation mediated through rat spinal 5HT3 receptors is unaltered following carrageenan inflammation. Rahman, W., Suzuki, R., Rygh, L.J., Dickenson, A.H. Neurosci. Lett. (2004) [Pubmed]
  33. Postoperative delirium indicating an adverse drug interaction involving the selective serotonin reuptake inhibitor, paroxetine? Stanford, B.J., Stanford, S.C. J. Psychopharmacol. (Oxford) (1999) [Pubmed]
  34. The polymorphic cytochrome P-4502D6 is involved in the metabolism of both 5-hydroxytryptamine antagonists, tropisetron and ondansetron. Fischer, V., Vickers, A.E., Heitz, F., Mahadevan, S., Baldeck, J.P., Minery, P., Tynes, R. Drug Metab. Dispos. (1994) [Pubmed]
  35. Ondansetron for patients given abdominal radiotherapy. Rosenthal, S.A., Marquez, C.M., Hourigan, H.P., Ryu, J.K. Lancet (1992) [Pubmed]
  36. Review of the preclinical pharmacology and comparative efficacy of 5-hydroxytryptamine-3 receptor antagonists for chemotherapy-induced emesis. Perez, E.A. J. Clin. Oncol. (1995) [Pubmed]
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