| 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
(Affiliation: Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka, Japan.)
|
| Journal | Nippon yakurigaku zasshi. Folia pharmacologica Japonica
(Nippon Yakurigaku Zasshi)
Vol. 98
Issue 4
Pg. 293-9
(Oct 1991)
ISSN: 0015-5691 JAPAN |
| PMID | 1802816
(Publication Type: Comparative Study, English Abstract, Journal Article)
|
| Chemical References |
- Bicyclo Compounds
- Bicyclo Compounds, Heterocyclic
- Oxazines
- Receptors, Serotonin
- azasetron
- Metoclopramide
- Serotonin
- 2-methyl-5-HT
|
| Topics |
- Anesthesia
- Animals
- Bicyclo Compounds
(pharmacology)
- Bicyclo Compounds, Heterocyclic
- Heart Rate
(drug effects)
- Male
- Metoclopramide
(pharmacology)
- Oxazines
(pharmacology)
- Rats
- Rats, Inbred Strains
- Receptors, Serotonin
(drug effects)
- Serotonin
(analogs & derivatives, pharmacology)
|
