The potential anxiolytic activity of GR38032F, a 5-HT3-receptor antagonist

Br J Pharmacol. 1988 Apr;93(4):985-93. doi: 10.1111/j.1476-5381.1988.tb11489.x.


1. The highly selective 5-HT3-receptor antagonist, GR38032F, has been tested in five animal models predictive for anxiolytic activity. 2. In the social interaction test in the rat and in a light/dark exploration test in the mouse, GR38032F dose-dependently released suppressed behaviour without modifying locomotor activity. 3. In the cynomolgus monkey and the marmoset, GR38032F reduced anxiety-related symptoms without causing sedation. In the marmoset, the effects were clearly dose-related. 4. GR38032F did not have any detectable activity in the water-lick conflict test in the rat. 5. We conclude that GR38032F is potentially a very potent anxiolytic agent without sedative, anticonvulsant or hypnotic activity.

MeSH terms

  • Animals
  • Anti-Anxiety Agents*
  • Anticonvulsants
  • Callitrichinae
  • Conflict, Psychological
  • Female
  • Imidazoles / pharmacology*
  • Macaca mulatta
  • Male
  • Mice
  • Mice, Inbred Strains
  • Ondansetron
  • Pentobarbital / pharmacology
  • Pentylenetetrazole / antagonists & inhibitors
  • Radioligand Assay
  • Rats
  • Receptors, Serotonin / drug effects*
  • Sleep / drug effects


  • Anti-Anxiety Agents
  • Anticonvulsants
  • Imidazoles
  • Receptors, Serotonin
  • Ondansetron
  • Pentobarbital
  • Pentylenetetrazole