title: Endothelin receptor subtype(s) in rabbit jugular vein smooth muscle.
abstract: The goal of our study was to characterize pharmacologically the receptor subtype(s) that mediate endothelin-induced force development in the rabbit jugular vein. Endothelin-1 (ET-1), sarafotoxin S6c, and the linear endothelin peptide Ala11,15-ET-1[8-21] evoked approximately monophasic concentration-dependent increases in force development in the rabbit jugular vein (rank order of potency: sarafotoxin S6c > ET-1 > Ala11,15-ET-1[8-21]). Maximally effective concentrations of the relatively ETB-selective (in comparison to ETA) ligands sarafotoxin S6c and Ala11,15-ET-1[8-21] produced significantly less force than a maximally effective ET-1 concentration (79 and 78% of ET-1 max., respectively; p < 0.001 for both). ET-3 produced a relatively shallow concentration-force relationship. Force evoked by ET-1 was minimally affected by the relatively ETA-selective (in comparison with ETB) receptor antagonists BQ-123 and FR139317. These data indicate that the dominant functional ET receptor in rabbit jugular vein smooth muscle is of a non-ETA subtype.
authors.affiliation: Department of Pharmacology, Bristol-Myers Squibb PRI, Princeton, NJ 08543-4000.
authors.forename: N J
authors.initials: NJ
authors.lastname: Lodge
authors.forename: N N
authors.initials: NN
authors.lastname: Halaka
mesh_terms: D000818:Animals; D001381:Azepines / Q000494:pharmacology; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000494:pharmacology; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology; D007601:Jugular Veins / Q000378:metabolism; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects / Q000502:physiology; D009131:Muscle, Smooth, Vascular / Q000378:metabolism*; D010456:Peptides, Cyclic / Q000494:pharmacology; D011817:Rabbits; D017466:Receptors, Endothelin / Q000378:metabolism*; D014757:Viper Venoms / Q000494:pharmacology
chemical_list: D001381:Azepines; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D007211:Indoles; D010456:Peptides, Cyclic; D017466:Receptors, Endothelin; D014757:Viper Venoms; C057354:sarafotoxins s6; C079574:FR 139317; C072247:cyclo(Trp-Asp-Pro-Val-Leu)