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

Bermudez, J.; Sanger, G.J.

Journal of Pharmacy and Pharmacology 46(6): 520-521

1994

ISSN/ISBN: 0022-3573
PMID: 7932054
Document Number: 426956
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-HT-3 receptor in-vivo.

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