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Chemical Compound Review

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

Synonyms: Emetron, Ondemet, Emeset, PubChem17490, SureCN41455, ...
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Disease relevance of Zofran


Psychiatry related information on Zofran

  • In a third experiment, the effects of GR 38032F (0.1 and 1 mg/kg, oral) and zacopride (0.01, 0.1 and 1 mg/kg, oral) were investigated in the high light test conditions of the social interaction test; neither compound had a significant effect [6].

High impact information on Zofran


Biological context of Zofran

  • 4. IC50 values for ICS 205-930, GR 38032F, MDL 72222, cocaine and curare in inhibiting the nicotinic depolarizations were 4 microM, 12 microM, 11 microM, 6 microM and 17 microM, respectively [12].

Associations of Zofran with other chemical compounds


Gene context of Zofran

  • The postprandial integrated response and peak release of PYY was decreased by GR 38032F [18].
  • Prior intraperitoneal administration of the 5-HT3 receptor antagonists ICS 205-930 or GR 38032F (0.05-2.5 mg/kg i.p.) inhibited the restraint stress-induced PRL release dose-dependently [19].
  • Blockade of 5-HT3 receptors by GR 38032F (10(-6) M) did not affect the potentiation by 5-HT [20].
  • Mean total colonic transit time on placebo was 27.8 hr, while on GR 38032F it was 39.1 hr (P less than 0.0005) [21].

Analytical, diagnostic and therapeutic context of Zofran

  • To determine if GR 38032F, a selective 5HT3 antagonist known to have antiemetic effects, influences colonic transit in health, a randomized, double-blind, placebo-controlled crossover study was performed [21].


  1. 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]
  2. GR 38032F (GR-C507/75): a novel compound effective in the prevention of acute cisplatin-induced emesis. Hesketh, P.J., Murphy, W.K., Lester, E.P., Gandara, D.R., Khojasteh, A., Tapazoglou, E., Sartiano, G.P., White, D.R., Werner, K., Chubb, J.M. J. Clin. Oncol. (1989) [Pubmed]
  3. Evaluation of three oral dosages of ondansetron in the prevention of nausea and emesis associated with cyclophosphamide-doxorubicin chemotherapy. Fraschini, G., Ciociola, A., Esparza, L., Templeton, D., Holmes, F.A., Walters, R.S., Hortobagyi, G.N. J. Clin. Oncol. (1991) [Pubmed]
  4. Serotonin 5-HT3-receptor antagonist GR 38032F suppresses sleep apneas in rats. Radulovacki, M., Trbovic, S.M., Carley, D.W. Sleep. (1998) [Pubmed]
  5. The effect on motion sickness and oculomotor function of GR 38032F, a 5-HT3-receptor antagonist with anti-emetic properties. Stott, J.R., Barnes, G.R., Wright, R.J., Ruddock, C.J. British journal of clinical pharmacology. (1989) [Pubmed]
  6. Lack of effects of 5HT3 receptor antagonists in the social interaction and elevated plus-maze tests of anxiety in the rat. File, S.E., Johnston, A.L. Psychopharmacology (Berl.) (1989) [Pubmed]
  7. Antiemetic efficacy and pharmacokinetic analyses of the serotonin antagonist ondansetron (GR 38032F) during multiple-day chemotherapy with cisplatin prior to autologous bone marrow transplantation. Lazarus, H.M., Bryson, J.C., Lemon, E., Pritchard, J.F., Blumer, J. J. Natl. Cancer Inst. (1990) [Pubmed]
  8. Effects of cisapride on cholinergic neurotransmission and propulsive motility in the guinea pig ileum. Tonini, M., Galligan, J.J., North, R.A. Gastroenterology (1989) [Pubmed]
  9. Antagonism of serotonin S3 receptors with ondansetron prevents nausea and emesis induced by cyclophosphamide-containing chemotherapy regimens. Cubeddu, L.X., Hoffman, I.S., Fuenmayor, N.T., Finn, A.L. J. Clin. Oncol. (1990) [Pubmed]
  10. Identification of serotonin 5-HT3 recognition sites in membranes of N1E-115 neuroblastoma cells by radioligand binding. Hoyer, D., Neijt, H.C. Mol. Pharmacol. (1988) [Pubmed]
  11. Ondansetron. Therapeutic use as an antiemetic. Milne, R.J., Heel, R.C. Drugs (1991) [Pubmed]
  12. Effects of 5-HT3 receptor antagonists on 5-HT and nicotinic depolarizations in guinea-pig submucosal neurones. Vanner, S., Surprenant, A. Br. J. Pharmacol. (1990) [Pubmed]
  13. The gastrointestinal prokinetic benzamide derivatives are agonists at the non-classical 5-HT receptor (5-HT4) positively coupled to adenylate cyclase in neurons. Dumuis, A., Sebben, M., Bockaert, J. Naunyn Schmiedebergs Arch. Pharmacol. (1989) [Pubmed]
  14. Comparison of the cardiovascular effects of the 5-HT1A receptor agonist flesinoxan with that of 8-OH-DPAT in the rat. Dreteler, G.H., Wouters, W., Saxena, P.R. Eur. J. Pharmacol. (1990) [Pubmed]
  15. Involvement of 5-HT1, 5-HT2, and 5-HT3 receptors in the mediation of the prolactin response to serotonin and 5-hydroxytryptophan. Jørgensen, H., Knigge, U., Warberg, J. Neuroendocrinology (1992) [Pubmed]
  16. Comparison of ondansentron (GR 38032F) versus ondansentron plus alprazolam as antiemetic prophylaxis during cisplatin-containing chemotherapy. Tsavaris, N., Charalambidis, G., Pagou, M., Karabelis, A., Mylonakis, N., Bacoyiannis, C., Kosmidis, P. Am. J. Clin. Oncol. (1994) [Pubmed]
  17. Modulation of baseline behavior in rats by putative serotonergic agents in three ethoexperimental paradigms. Kshama, D., Hrishikeshavan, H.J., Shanbhogue, R., Munonyedi, U.S. Behavioral and neural biology. (1990) [Pubmed]
  18. Effect of selective 5HT3 antagonist (GR 38032F) on small intestinal transit and release of gastrointestinal peptides. Talley, N.J., Phillips, S.F., Haddad, A., Miller, L.J., Twomey, C., Zinsmeister, A.R., Ciociola, A. Dig. Dis. Sci. (1989) [Pubmed]
  19. Effect of serotonin 5-HT1, 5-HT2, and 5-HT3 receptor antagonists on the prolactin response to restraint and ether stress. Jørgensen, H., Knigge, U., Warberg, J. Neuroendocrinology (1992) [Pubmed]
  20. 5-HT1-like receptors mediate potentiation of cholinergic nerve-mediated contraction of isolated mouse trachea. Van Oosterhout, A.J., Hofman, G., Woutersen-Van Nijnanten, F.M., Nijkamp, F.P. Eur. J. Pharmacol. (1991) [Pubmed]
  21. GR 38032F (ondansetron), a selective 5HT3 receptor antagonist, slows colonic transit in healthy man. Talley, N.J., Phillips, S.F., Haddad, A., Miller, L.J., Twomey, C., Zinsmeister, A.R., MacCarty, R.L., Ciociola, A. Dig. Dis. Sci. (1990) [Pubmed]
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