Journal of Smooth Muscle Research · 1998 · 12 citations · 15 references
MedicinePharmacologyGeneral PharmacologyNeuropharmacologyPharmacodynamicsRabbit PharmacologySerotonergic Pharmacology5-Hydroxytryptamine Receptor PharmacologyCyclooxygenase InhibitorsDirect Smooth Muscle RelaxantsNitric OxideProstanoid SignalingReceptorsVascular Smooth Muscle PharmacologyVascular Smooth Muscle Relaxation
The facial vein in several species has been shown to have unusual properties, including exhibition of spontaneous myogenic tone and relaxation to norepinephrine (NE). The present study was undertaken to characterize the relaxant effect of 5-hydroxytryptamine (5-HT) on the rabbit facial vein. An isolated ring preparation of the rabbit facial vein exhibited intrinsic tone when it was stretched and the spontaneous contraction continued for hours. 5-HT concentration-dependently relaxed facial veins exhibiting spontaneous contraction. The relaxation was not inhibited by rubbing the endothelium or by NG-nitro-L-arginine (10(-4) M), a nitric oxide (NO) synthase inhibitor. The 5-HT-induced relaxation was also unaffected by pretreatment with indomethacin (10(-5) M), a cyclooxygenase inhibitor, and propranolol (10(-6) M), a both beta-adrenoceptor and 5-HT18-receptor antagonist. In contrast, 5-HT-induced relaxation of the facial vein was concentration-dependently antagonized by methysergide (10(-7) M and 10(-6) M), a non-selective 5-HT1- and 5-HT2-receptor antagonist, but not by NAN-190 (10(-6) M) and SDZ-205,557 (10(-6) M), antagonists for 5-HT1A- and 5-HT4-receptors, respectively. A higher (10(-6) M), but not lower (3 x 10(-7) M) concentration of ketanserin, a 5-HT2-receptor antagonist, slightly inhibited the 5-HT-induced relaxation. These results indicate that 5-HT-induced relaxation is not due to indirect mechanisms mediated by NE released from the sympathetic nerve terminals, or by endogenous prostanoid and endothelium-derived relaxing factor (EDRF = NO) released from the vascular tissues, but due to a direct effect on the 5-HT receptors located on vascular smooth muscle cells. However, the subtype of 5-HT receptor that produces relaxation of the rabbit facial vein remains to be clarified.
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Proposals for the classification and nomenclature of functional receptors for 5-hydroxytryptamine
Philip Bradley, G. Engel, W. Feniuk et al. · Neuropharmacology · 1986 · 1.3K citations
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Pharmacologic Analysis of Drug Receptor Interaction
Kenakin. T. Kenakin · Therapeutic Drug Monitoring · 1988 · 930 citations
Philippe Schoeffter, Daniël Hoyer · British Journal of Pharmacology · 1988 · 150 citations · Full text
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Endothelium-derived vascular relaxing factor.
M J Peach, Alex L. Loeb, Harold A. Singer et al. · Hypertension · 1985 · 117 citations · Full text