Sumatriptan is an agonist at 5-HT1Preceptors on myenteric neurones in the guinea-pig gastric antrum
| Autor: | P. Vanden Berghe, Bernard Coulie, Jozef Janssens, Jan Tack |
|---|---|
| Rok vydání: | 2007 |
| Předmět: |
Agonist
medicine.medical_specialty Endocrine and Autonomic Systems Physiology medicine.drug_class Chemistry Gastroenterology Gastric motility Pharmacology musculoskeletal system Renzapride Sumatriptan Endocrinology Internal medicine cardiovascular system medicine Cholinergic Enteric nervous system Antrum 5-HT receptor medicine.drug |
| Zdroj: | Neurogastroenterology & Motility. 19:39-46 |
| ISSN: | 1365-2982 1350-1925 |
| Popis: | Sumatriptan, a 5-hydroxytryptamine(1D) (5-HT(1D))-receptor agonist used in the treatment in migraine, inhibits gastric motility via the enteric nervous system. As no studies have reported enteric neuronal 5-HT(1D) receptors, we used conventional intracellular recordings to characterize the actions of sumatriptan on 145 guinea-pig antral myenteric neurones. In 24 of 29 neurones with a 5-HT(1P) receptor-mediated depolarizing response to 5-HT, application of sumatriptan caused a dose-dependent depolarization, accompanied by increased membrane resistance and enhanced excitability. Depolarizing responses to sumatriptan occurred both in cholinergic and in nitrergic neurones. Sumatriptan did not mimic the 5-HT(3) receptor-mediated fast-depolarizing responses or 5-HT(1A) receptor-mediated inhibitory responses to 5-HT. Sumatriptan had no effect on neurones not responding to 5-HT. The depolarizing response to sumatriptan was inhibited by renzapride, but not by 5-HT(1-7) receptor antagonists. We conclude that sumatriptan behaves as an agonist at the 5-HT(1P) receptor on myenteric neurones in the guinea-pig gastric antrum. The actions of sumatriptan on gastric motility seem to be attributable to a direct action on enteric neurones. |
| Databáze: | OpenAIRE |
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