Antiemetic effects of serotonergic 5-HT1A-receptor agonists in Suncus murinus.
The antiemetic effects of six serotonergic 5-HT1A-receptor agonists, 8-hydroxy-2-(di-n-propylamino)tetrarin (8-OH-DPAT), 4-(4-[4-(2-pyrimidinyl)piperazin-1-yl]butyl)-2,3,4,5- tetrahydro-1,4-benzoxazepine-3,5-dione (SUN8399), buspirone, gepirone, ipsapirone and tandospirone, against motion sickness were investigated in Suncus murinus. Subcutaneous injection of all six agonists completely and dose-dependently suppressed motion-induced emesis. Pretreatment with 8-OH-DPAT or SUN8399 dose-dependently inhibited emesis elicited by nicotine (4.0 mg/kg, s.c.), veratrine (0.7 mg/kg, s.c.), cisplatin (20 mg/kg, i.p.) and copper sulfate (40 mg/kg, p.o.). These results suggest that serotonergic 5-HT1A-receptor agonists are effective as anti-motion sickness drugs, and these drugs may block a common mechanism(s) for the emetic reflex of the suncus because the antiemetic effects of the 5-HT1A-receptor agonists were exerted irrespective of the stimulus.
Okada
F
F
Department of Chemical Pharmacology, Faculty of Pharmaceutical Science, University of Tokyo, Japan.
Torii
Y
Y
Saito
H
H
Matsuki
N
N
D017371:8-Hydroxy-2-(di-n-propylamino)tetralin / Q000494:pharmacology; D000818:Animals; D000932:Antiemetics / Q000494:pharmacology*; D002065:Buspirone / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D008297:Male; D009041:Motion Sickness / Q000517:prevention & control*; D010077:Oxazepines / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000494:pharmacology*; D012788:Shrews / Q000502:physiology*; D014839:Vomiting / Q000139:chemically induced / Q000517:prevention & control
D000932:Antiemetics; D010077:Oxazepines; D017366:Serotonin Receptor Agonists; C088257:SUN 8399; D017371:8-Hydroxy-2-(di-n-propylamino)tetralin; D002065:Buspirone