Effects of Mosapride Citrate, a 5-HT4 Receptor Agonist, on Colonic Motility in Conscious Guinea Pigs
| Autor: | Ryuji Nagai, Tsugutaka Ito, Atsuko Inui, Takashi Yoshikawa, Naoyuki Yoshida |
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| Rok vydání: | 2002 |
| Předmět: |
Male
Agonist medicine.medical_specialty Time Factors Colon medicine.drug_class Morpholines Guinea Pigs Methysergide 5-HT4 receptor Dioxanes Radioligand Assay Piperidines Internal medicine medicine Animals Receptor Pharmacology Dose-Response Relationship Drug Chemistry Antagonist Mosapride Serotonin Receptor Agonists Atropine Endocrinology Cisapride Receptors Serotonin Benzamides Autoradiography Serotonin Antagonists Gastrointestinal Motility medicine.drug |
| Zdroj: | Japanese Journal of Pharmacology. 90:313-320 |
| ISSN: | 0021-5198 |
| DOI: | 10.1254/jjp.90.313 |
| Popis: | It is known that 5-HT(4) receptors in the colon of guinea pigs show a distribution similar to that in humans. Thus, we examined the effects of mosapride citrate (mosapride) and cisapride, two 5-HT(4)-receptor agonists, on colonic motility in conscious guinea pigs implanted with force transducers. Mosapride and cisapride administered intragastrically at doses of 3 - 30 mg/kg significantly enhanced the colonic motility. The enhancing effect of mosapride was antagonized by atropine or GR113808, a 5-HT(4)-receptor antagonist, but not by methysergide, a 5-HT(1)- and 5-HT(2)-receptor antagonist; ondansetron, a 5-HT(3)-receptor antagonist; or CP-99994, a tachykinin NK(1)-receptor antagonist. In vitro receptor autoradiography showed that mosapride and cisapride inhibit the specific binding of [(125)I]-SB207710, a selective radioligand of 5-HT(4) receptors, in the colon of guinea pigs. These results suggest that mosapride enhances colonic motility through the 5-HT(4)-receptor activation in guinea pigs and may be useful for treating constipation in patients with colonic motility dysfunction. |
| Databáze: | OpenAIRE |
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