[Inhibition by Y-25130 of the von Bezold-Jarisch effect evoked by 5-HT or 2-methyl-5-HT in anesthetized rats].

Abstract

Effect of Y-25130 on 5-hydroxytryptamine3 (5-HT3) receptors was investigated using the von Bezold-Jarisch effect (BJE) in anesthetized rats. Intravenous or intraduodenal administration of Y-25130 antagonized the BJE evoked by 5-HT and its effect was over 100 times more potent than that of metoclopramide. Y-25130 also completely blocked the BJE induced by 2-methyl-5-HT, a selective 5-HT3 receptor agonist. The BJE induced by 5-HT was not antagonized by spiperone, ketanserin, phenoxybenzamine, yohimbine and haloperidol, but antagonized by atropine. Atropine inhibited the bradycardia caused by electrical stimulation of the vagus nerve, but Y-25130 had no inhibitory effect. These results indicate that Y-25130 possesses a potent and selective 5-HT3 receptor antagonistic property.

• Authors: K Inaba, Y Morimoto, T Fukuda, M Setoguchi
• Journal: Nihon yakurigaku zasshi. Folia pharmacologica Japonica (Nihon Yakurigaku Zasshi) Vol. 98 Issue 4 Pg. 293-9 (Oct 1991) ISSN: 0015-5691 [Print] Japan
• PMID: 1802816 (Publication Type: Comparative Study, Journal Article)

Chemical References

• Bridged Bicyclo Compounds
• Bridged Bicyclo Compounds, Heterocyclic
• Oxazines
• Receptors, Serotonin
• Serotonin
• azasetron
• 2-methyl-5-HT
• Metoclopramide

Topics

• Anesthesia
• Animals
• Bridged Bicyclo Compounds (pharmacology)
• Bridged Bicyclo Compounds, Heterocyclic
• Heart Rate (drug effects)
• Male
• Metoclopramide (pharmacology)
• Oxazines (pharmacology)
• Rats
• Rats, Inbred Strains
• Receptors, Serotonin (drug effects)
• Serotonin (analogs & derivatives, pharmacology)