caa a22 4500 469078529 CHVBK 20180323132942.0 cr unu---uuuuu 170328e19921101xx s 000 0 eng 10.1007/BF00169018 doi (NATIONALLICENCE)springer-10.1007/BF00169018 Sumatriptan contracts large coronary arteries of beagle dogs through 5-HT1-like receptors [Elektronische Daten] [Andrew Parsons, Cathy Stutchbury, Pravin Raval, Alberto Kaumann] Summary: The effects of 5-hydroxytryptamine (5-HT), 5-carboxamidotryptamine (5-CT), methysergide and sumatriptan were studied on endothelium-denuded rings of beagle dog large coronary arteries. Submicromolar concentrations of the compounds contracted the rings with the order of potency 5-CT > 5-HT >sumatriptan = methysergide. Concentrations greater than 2 μM of both 5-HT and 5-CT, and 60 μmol/l methysergide also caused concentration-dependent relaxation. Sumatriptan did not cause relaxation. Peak intrinsic activities relative to the plateau contraction to sumatriptan (1.00), were 5-CT 0.47, 5-HT 0.87 and methysergide 0.51. Ketanserin 1 μmol/l affected neither contractile responses nor relaxant responses to 5-CT, methysergide and sumatriptan and only caused marginal blockade of the contractile effects of 5-HT. Methiothepin 200 nM shifted the concentration-contractile response curves by around 2 log units, as expected from its affinity for 5-HT1-like receptors. The rank order of contractile potency of the agonists, the antagonism by methiothepin and the resistance to blockade by ketanserin are consistent with a nearly exclusive involvement of 5-HT1-like receptors. Isolated large coronary arteries from beagle dogs may be a suitable model for the study of human coronary artery 5-HT1-like receptors that are involved in the spasm observed with 5-HT and sumatriptan. Springer-Verlag, 1992 Beagle dog large coronary arteries nationallicence 5-HT1-like receptors nationallicence 5-hydroxytryptamine nationallicence Sumatriptan nationallicence Model coronary spasm nationallicence Parsons Andrew Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut Stutchbury Cathy Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut Raval Pravin Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut Kaumann Alberto Clinical Pharmacology Unit, Cambridge University, Addenbrooke's Hospital, CB2 2QQ, Cambridge, UK aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/5(1992-11-01), 592-596 0028-1298 346:5<592 1992 346 210 https://doi.org/10.1007/BF00169018 text/html Onlinezugriff via DOI 1 brief-communication jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00169018 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Parsons Andrew Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut NATIONALLICENCE 700 1- Stutchbury Cathy Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut NATIONALLICENCE 700 1- Raval Pravin Smith Kline Beecham Pharmaceuticals. The Frythe, Welwyn, AL6 9AR, Herts, United Kingdom aut NATIONALLICENCE 700 1- Kaumann Alberto Clinical Pharmacology Unit, Cambridge University, Addenbrooke's Hospital, CB2 2QQ, Cambridge, UK aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 346/5(1992-11-01), 592-596 0028-1298 346:5<592 1992 346 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer