Cisapride, a gastroprokinetic agent, binds to 5-HT4 receptors
| Autor: | Keiichiro Haga, Yasunori Morio, Takemi Fukuda, Ken-ichi Katayama |
|---|---|
| Rok vydání: | 1995 |
| Předmět: |
Male
medicine.medical_specialty Metoclopramide Guinea Pigs BIMU8 In Vitro Techniques Pharmacology Binding Competitive Guinea pig Zacopride chemistry.chemical_compound Piperidines Internal medicine medicine Animals Receptor Cisapride Dose-Response Relationship Drug Chemistry musculoskeletal system Mosapride Serotonin Receptor Agonists Dose–response relationship Endocrinology Receptors Serotonin Serotonin Antagonists medicine.drug |
| Zdroj: | Folia Pharmacologica Japonica. 105:461-468 |
| ISSN: | 1347-8397 0015-5691 |
| DOI: | 10.1254/fpj.105.461 |
| Popis: | The affinity of cisapride for 5-HT4 receptors was investigated in comparison with those of other 5-HT4 receptor agonists and antagonists, such as 5-HT, 5-MeOT, mosapride, zacopride, metoclopramide, BIMU8, GR113808, SDZ 205-557 and ICS 205-930. Cisapride and the other compounds dose-dependently inhibited specific 3H-GR113808 binding to 5-HT4 receptors in guinea pig striatal membranes, and complete inhibition of specific 3H-GR113808 binding was achieved at the high concentrations of these compounds. Cisapride was 1.9-, 7.3-, 4.3-, 11- and 26-fold more potent than 5-HT, 5-MeOT, mosapride, zacopride and metoclopramide, respectively, in competing for 5-HT4 receptors. To determine the manner of interaction between cisapride and 5-HT4 receptors, Scatchard analysis of 3H-GR113808 specific binding to striatal membranes was performed. Cisapride increased the Kd value of 3H-GR113808 in striatal membranes in a dose-dependent manner without any influence on the binding density (Bmax) of 3H-GR113808. These findings indicate that cisapride binds to 5-HT4 receptors competing with 3H-GR113808 in guinea pig striatal membranes. |
| Databáze: | OpenAIRE |
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