5-Hydroxytryptamine (5-HT) contracts the guinea-pig isolated iliac artery via 5-HT1-like and 5-HT2 receptors.
The characterization of 5-hydroxytryptamine (5-HT) receptors mediating contractions of the guinea-pig isolated iliac artery was studied when the basal tone was slightly increased by prostaglandin F2 alpha (PGF2 alpha). In the presence of ketanserin (1 mumol/l), 5-HT and several 5-HT receptor agonists induced contractile responses with the rank order of agonist potency: 5-HT = 5-carboxyamidotryptamine (5-CT) = lysergol > ergometrine = methylergometrine > RU 24969 approximately 5-methoxytryptamine (5-MeOT) > methysergide > sumatriptan > tryptamine. Concentration-effect curves to the ergot alkaloids, lysergol, ergometrine, methylergometrine and methylsergide, were biphasic. In the presence of ketanserin (1 mumol/l), contractile responses to 5-HT, 5-CT, RU 24969, 5-MeOT, sumatriptan and tryptamine were antagonized by methiothepin (30 nmol/l) and flesinoxan (3 mumol/l) with approximate pKB values of 8.5-9.0 and 6.0-6.3, respectively. The first phase of contraction produced by the ergot alkaloids, lysergol, ergometrine, methylergometrine and methysergide, were blocked by methiothepin (30 nmol/l) and flesinoxan (3 mumol/l), respectively, with approximate pKB values about 8.4-8.7 and 6.2-6.4, respectively. The mechanism underlying the second phase of contraction remains to be established. Maximum responses of the concentration-effect curves to 5-HT (1 nmol/l-1 mumol/l) were concentration-dependently depressed by ketanserin (1 nmol/l-1 mumol) and spiperone (30 nmol/l-0.3 mumol/l) and reached approximately 60% of the 5-HT maximum response in the presence of ketanserin (1 mumol/l) and spiperone (0.1 mumol/l), respectively. Agonist potency of 5-HT was not affected by the antagonists.(ABSTRACT TRUNCATED AT 250 WORDS)
Pertz
H
H
Fachbereich Pharmazie, Freie Universität Berlin, Germany.
D000818:Animals; D015237:Dinoprost / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D007083:Iliac Artery / Q000187:drug effects; D066298:In Vitro Techniques; D007650:Ketanserin / Q000494:pharmacology; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D011985:Receptors, Serotonin / Q000187:drug effects*; D012701:Serotonin / Q000494:pharmacology*; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists / Q000494:pharmacology
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D012701:Serotonin; D007650:Ketanserin; D015237:Dinoprost