European journal of pharmacology, 2000-09, Vol.404 (3), p.361-368
2000
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Details
- Autor(en) / Beteiligte
- Titel
- Effects of SL 65.0472, a novel 5-HT receptor antagonist, on 5-HT receptor mediated vascular contraction
- Ist Teil von
- European journal of pharmacology, 2000-09, Vol.404 (3), p.361-368
- Ort / Verlag
- Amsterdam: Elsevier B.V
- Erscheinungsjahr
- 2000
- Quelle
- Elsevier Journal Backfiles on ScienceDirect (DFG Nationallizenzen)
- Beschreibungen/Notizen
- 5-Hydroxytryptamine (5-HT) contracts vascular smooth muscle and pharmacological and molecular biological data suggest that these effects are mediated primarily by stimulation of 5-HT 1B and 5-HT 2A receptor subtypes. We have studied the properties of 7-fluoro-2-oxo-4-[2-[4-(thieno[3,2- c] pyridin-4-yl) piperazin-1-yl] ethyl]-1,2-dihydroquinoline-1-acetamide (SL 65.0472 ), a novel 5-HT receptor antagonist, in isolated vascular preparations contracted by 5-HT or sumatriptan. In canine isolated saphenous vein strips (putatively 5-HT 1B-mediated contraction), SL 65.0472 antagonised sumatriptan-induced contractions in a competitive manner (p A 2 8.17±0.36). 5-HT contracts rabbit aorta by stimulation of 5-HT 2A receptors. SL 65.0472 displaced the 5-HT concentration response curve in rabbit aorta rightwards with a significant reduction in maximum. The apparent p K B value was 8.58±0.18. 5-HT-induced contractions of human coronary arteries are mediated by a mixed population of 5-HT 1B and 5-HT 2A receptors. SL 65.0472 produced rightward parallel shifts of the 5-HT concentration response curves in all tissues studied (p A 2 8.8±0.14, n=7). In conclusion, SL 65.0472 is a potent antagonist of vascular smooth muscle contraction in vitro mediated by 5-HT receptor stimulation.
- Sprache
- Englisch
- Identifikatoren
- ISSN: 0014-2999eISSN: 1879-0712DOI: 10.1016/S0014-2999(00)00630-0Titel-ID: cdi_proquest_miscellaneous_72282932
- Format
- –
- Schlagworte
- 5-HT 1B receptor, 5-HT 2A receptor, Animals, Aorta - drug effects, Aorta - physiology, Biological and medical sciences, Cardiovascular system, Coronary Vessels - drug effects, Coronary Vessels - physiology, Dogs, Female, Free Radical Scavengers - pharmacology, Humans, Male, Medical sciences, Pharmacology. Drug treatments, Piperazines - chemistry, Piperazines - pharmacology, Quinolines - chemistry, Quinolines - pharmacology, Rabbits, Receptor, Serotonin, 5-HT1B, Receptor, Serotonin, 5-HT2A, Receptors, Serotonin - drug effects, Receptors, Serotonin - physiology, Saphenous Vein - drug effects, Saphenous Vein - physiology, Serotonin - pharmacology, Serotonin Antagonists - chemistry, Serotonin Antagonists - pharmacology, SL 65.0472, Sumatriptan - pharmacology, Vasoconstriction, Vasoconstriction - drug effects, Vasoconstriction - physiology, Vasoconstrictor Agents - pharmacology, Vasodilator agents. Cerebral vasodilators