Evidence for 5-HT1-like receptor-mediated vasoconstriction in human pulmonary artery
| Autor: | A.G.B. Templeton, Ian Morecroft, R.A. Clayton, Margaret R. MacLean |
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| Rok vydání: | 1996 |
| Předmět: |
Agonist
Serotonin medicine.medical_specialty Ketanserin Pyridines medicine.drug_class Methiothepin In Vitro Techniques Pulmonary Artery Internal medicine medicine Humans Receptor Pharmacology 8-Hydroxy-2-(di-n-propylamino)tetralin Chemistry Antagonist musculoskeletal system Receptor antagonist Serotonin Receptor Agonists Kinetics Sumatriptan Endocrinology Vasoconstriction Competitive antagonist Receptors Serotonin Benzamides cardiovascular system 5-HT1 receptor Serotonin Antagonists Research Article medicine.drug |
| Zdroj: | British Journal of Pharmacology. 119:277-282 |
| ISSN: | 0007-1188 |
| DOI: | 10.1111/j.1476-5381.1996.tb15982.x |
| Popis: | 1. The 5-hydroxytryptamine (5-HT) receptors mediating contraction of human isolated pulmonary artery rings were investigated. Responses to the agonists 5-carboximidotryptamine (5-CT, non-selective 5-HT1 agonist), sumatriptan (5-HT1D-like receptor agonist), 5-HT and 8-hydroxy-2-(di-n-propylamino)-tetralin (8-OH-DPAT, 5-HT1A receptor agonist) were studied. Responses to 5-HT and sumatriptan in the presence of the antagonists, methiothepin (non-selective 5-HT1+2-receptor antagonist), ketanserin (5-HT2A receptor antagonist) and the novel antagonist, GR55562 (5-HT1D receptor antagonist) were also studied. 2. All agonists contracted human pulmonary artery ring preparations in the following order of potency 5-CT > 5-HT = sumatriptan > 8-OH-DPAT. Maximum responses to 5-HT, 5-CT and sumatriptan were not significantly different. 3. Methiothepin 1 nM and 10 nM, but not 0.1 nM reduced the maximum contractile responses to 5-HT but did not alter tissue sensitivity to 5-HT. Methiothepin 0.1 nM, 1 nM and 10 nM had a similar effect on responses to sumatriptan. 4. The 5-HT2A receptor antagonist ketanserin (10 nM, 100 nM and 1 microM) also reduced the maximum contractile response to both 5-HT and sumatriptan without affecting tissue sensitivity to these agonists. 5. The novel 5-HT1D receptor antagonist, GR55562, inhibited responses to 5-HT and sumatriptan in a true competitive fashion. 6. The results suggest that the human pulmonary artery has a functional population of 5-HT1D-like receptors which are involved in the contractile response to 5-HT. |
| Databáze: | OpenAIRE |
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