Effect of Zatosetron on Ipecac‐Induced Emesis in Dogs and Healthy Men

  title={Effect of Zatosetron on Ipecac‐Induced Emesis in Dogs and Healthy Men},
  author={Steven M. Schwartz and Mark J. Goldberg and Jaswant S. Gidda and Benito J. Cerimele},
  journal={The Journal of Clinical Pharmacology},
Serotonin receptor (5‐HT3) antagonists provide effective antiemetic therapy in cancer patients receiving emetogenic chemotherapy, such as cisplatin. Animal studies have shown that 5‐HT3 receptor antagonists also have antiemetic activity in ipecac‐induced emesis. The authors investigated the antiemetic activity of zatosetron maleate, a 5‐HT3 receptor antagonist, on ipecac‐induced emesis in dogs and healthy men. They also evaluated the effect of ipecac administration on serotonin release and… 
Comparative efficacy of maropitant and selected drugs in preventing emesis induced by centrally or peripherally acting emetogens in dogs.
Maropitant was effective in preventing vomiting caused by stimulation of either central or peripheral emetic pathways, whereas the other drugs examined prevented vomiting causedBy central (metoclopramide and chlorpromazine) or peripheral (ondansetron; P < 0.0001) stimulation but not both.
Physiology of Chemotherapy-Induced Emesis and Antiemetic Therapy
Different animal and human models are available to study the physiology of emesis and to evaluate the antiemetic activity of new compounds, but they need to be predictors of clinical situations.
5-HT3 antagonists under development
Most drug candidates in clinical trials were discovered in the early 1990s and their patent expiry is imminent, so structurally diverse compound libraries need to be extensively investigated for identification of novel 5-HT3 receptor antagonists.
Pharmacological profile of LY301317, a potent and selective 5‐HT1A agonist
It was concluded that LY301317 is an orally active, potent, and selective agonist for the 5‐HT1A receptor with potential clinical utility as an anxiolytic, an antidepressant, and a broad‐spectrum antiemetic.
Blockade of phencyclidine-induced hyperlocomotion by olanzapine, clozapine and serotonin receptor subtype selective antagonists in mice
The present findings support the hypothesis that antagonism at 5-HT2A receptors contributes to the in vivo actions of atypical antipsychotics such as olanzapine and clozapine, and indicate that PCP increases locomotor activity, at least in part, due to actions at5- HT2A, but not 5- HT3 or5-HT1A, receptors.
Vomiting and Nausea


Efficacy of ondansetron (GR 38032F) and the role of serotonin in cisplatin-induced nausea and vomiting.
It is suggested that cisplatin treatment increases the release of serotonin from enterochromaffin cells, and that ondansetron acts by blocking S3 receptors for serotonin.
LY277359 maleate: a potent and selective 5-HT3 receptor antagonist without gastroprokinetic activity.
Several 5-hydroxytryptamine (5-HT3) receptor antagonists have been described. In addition to 5-HT3 receptor antagonist activity, many of these agents also possess gastroprokinetic activity. In the
Efficacy of ondansetron (GR38032F) and the role of serotomn in cisplatin-induced nausea and vomiting
  • N Engl J Med
  • 1990
LY277359 maleate: A potent and selective 5-HT3 antagonist without gastroprokinetic activity
  • J Pharmacol Exp Ther
  • 1990