F. Okada et al., BLOCKADE OF MOTION-INDUCED AND CISPLATIN-INDUCED EMESIS BY A 5-HT2 RECEPTOR AGONIST IN SUNCUS-MURINUS, British Journal of Pharmacology, 114(5), 1995, pp. 931-934
1 The effects of +/-)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane (D
Ol), a 5-hydroxytryptamine 5-HT2A/5-HT2C receptor agonist, on motion-
and cisplatin-induced emesis were studied in Suncus murinus. Subcutane
ous injection of DOl, 30 min prior to the emetic stimuli, dose-depende
ntly blocked the emesis induced by motion sickness and cisplatin (20 m
g kg(-1), i.p.) with estimated ID50 values of 640 and 780 mu g kg(-1),
respectively. 2 alpha-Methyl-5-hydroxytryptamine (alpha-Me-5-HT), a p
eripheral 5-HT2A/5-HT2C receptor agonist, had no effect on motion- and
cisplatin-induced emesis. 3 The antiemetic effects of DOl on motion-
and cisplatin-induced emesis were attenuated by preadministration of k
etanserin, a selective 5-HT2A receptor antagonist. 4 The present resul
ts suggest an inhibitory role for central 5-HT2 receptors in the emeti
c reflex mechanism and that a 5-HT2 receptor agonist may be a useful t
ool to investigate the involvement of 5-HT receptors in the emetic ref
lex.