5-HT1-like receptors mediate contractions of the rabbit saphenous vein.
5-Hydroxytryptamine (5-HT) elicited concentration-dependent contractions of the rabbit isolated saphenous vein. The effects of 5-HT were mimicked by 5-carboxamidotryptamine (5-CT), 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), 5-methoxy-3-(1,2,3,6-tetrahydro-4-pyridinyl)-1H-indole succinate (RU 24969) and sumatriptan; the rank order of potency (pD2 values) was 5-CT (7.6) greater than 5-HT (6.9) greater than 8-OH-DPAT (6.2) greater than RU 24969 (6.1) greater than sumatriptan (5.7). The maximal response to RU 24969 was less than that to the other compounds, implying that RU 24969 may behave as a partial agonist. Methiothepin (10(-8), 3 x 10(-8) and 3 x 10(-7) M), ketanserin (10(-7), 3 x 10(-7) and 10(-6) M) and spiperone (10(-7), 10(-6) and 10(-5) M), but not 1 alpha H,3 alpha,5 alpha H- tropan-3-yl-3,5-dichlorobenzoate (MDL 72222; 10(-7), 10(-6) or 10(-6) M), cyanopindolol (10(-7) and 10(-6) M) or propranolol (10(-7) and 10(-6) M), shifted the concentration-effect curve of 5-HT to the right in a concentration-dependent manner with pA2 values of 8.25, 7.51 and 6.12, respectively. The high activity of 5-CT and methiothepin compared to, respectively, 5-HT and ketanserin (and spiperone) suggests that the contraction of the rabbit saphenous vein is not mediated by 5-HT2 receptors. The receptor involved seems to be mainly 5-HT1-like, similar to the one mediating contraction of the dog saphenous vein, human basilar artery and porcine cranial arteriovenous anastomoses.
van Heuven-Nolsen
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Department of Pharmacology, Faculty of Medicine and Health Sciences, Erasmus University Rotterdam, The Netherlands.
Tysse Klasen
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Luo
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QF
Saxena
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PR
D000818:Animals; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000502:physiology; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D009638:Norepinephrine / Q000494:pharmacology; D011817:Rabbits; D011985:Receptors, Serotonin / Q000187:drug effects / Q000502:physiology*; D012501:Saphenous Vein / Q000502:physiology; D012701:Serotonin / Q000494:pharmacology; D012702:Serotonin Antagonists
D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D012701:Serotonin; D009638:Norepinephrine