Investigation of the 5-HT receptor mediating relaxation in guinea-pig proximal colon
| Autor: | C J Elswood, K T Bunce |
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| Rok vydání: | 1992 |
| Předmět: |
Agonist
Serotonin medicine.medical_specialty Metergoline Ketanserin Colon medicine.drug_class Muscle Relaxation Guinea Pigs Methysergide Pharmaceutical Science Tetrodotoxin In Vitro Techniques Biology Partial agonist chemistry.chemical_compound Internal medicine medicine Animals Receptor 5-HT receptor Pharmacology Muscle Smooth Endocrinology chemistry Receptors Serotonin Female Serotonin Antagonists medicine.drug |
| Zdroj: | Journal of Pharmacy and Pharmacology. 44:264-266 |
| ISSN: | 2042-7158 0022-3573 |
| DOI: | 10.1111/j.2042-7158.1992.tb03597.x |
| Popis: | 5-Hydroxytryptamine (5-HT) induced concentration-related relaxations (EC50 = 9·1 μm) of guinea-pig proximal colon pretreated with ketanserin (1 μm) and ondansetron (10 μm). This 5-HT-induced effect was neuronally mediated since it was blocked by tetrodotoxin (0·3 μm). 5-Carboxamidotryptamine was a full agonist and ten times more potent than 5-HT. α-Methyl-5-HT was a partial agonist. 2-Methyl-5-HT was without effect. Methysergide and metergoline were antagonists of 5-HT producing parallel shifts at 0·1 μm but unsurmountable antagonism at higher concentrations. pKB values of 8·0 and 7·3 were calculated for methysergide and metergoline, respectively. This study has identified a 5-HT-induced relaxation of guinea-pig proximal colon which is mediated via a neuronal 5-HT1-like receptor. However, the subtype has yet to be established. |
| Databáze: | OpenAIRE |
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