Prolonged anti-emetic activity and 5-HT3-receptor antagonism by BRL 46470 in conscious ferrets.

Abstract

The anti-emetic activity of oral and intravenously-administered BRL 46470 (endo-N-(8-methyl-8-azabicyclo[3.2.1]oct-3yl)-2,3-dihydro-3,3- dimethyl-indole-1-carboxamide HCl) has been assessed in conscious ferrets. BRL 46470 (0.05-0.5 mg kg-1, p.o.) dose-dependently prevented emesis evoked over a 2 h period by total body X-irradiation. This anti-emetic activity occurred with oral or intravenously-administered BRL 46470 even when dosed 3-4 h before radiation. In conjunction with data obtained in other species, we conclude that BRL 46470 has a potent and long-lasting ability to antagonize actions that are mediated by the 5-HT3 receptor in-vivo.

• Authors: J Bermudez, G J Sanger
• Journal: The Journal of pharmacy and pharmacology (J Pharm Pharmacol) Vol. 46 Issue 6 Pg. 520-1 (Jun 1994) ISSN: 0022-3573 [Print] England
• PMID: 7932054 (Publication Type: Journal Article)

Chemical References

• Antiemetics
• Bridged Bicyclo Compounds
• Bridged Bicyclo Compounds, Heterocyclic
• Indoles
• Serotonin Antagonists
• BRL 46470

Topics

• Administration, Oral
• Animals
• Antiemetics (pharmacology)
• Bridged Bicyclo Compounds (pharmacology)
• Bridged Bicyclo Compounds, Heterocyclic
• Dose-Response Relationship, Drug
• Ferrets
• Indoles (pharmacology)
• Injections, Intravenous
• Male
• Serotonin Antagonists (pharmacology)
• Whole-Body Irradiation