Venous smooth muscle contains vasoconstrictor ETB-like receptors.
Two endothelin (ET) receptor subtypes have been identified to date: the ETA receptor which preferentially binds ET-1 over ET-3, and the ETB receptor which is non-selective. This study characterized the ET receptor subtypes present in several vascular smooth muscle preparations using standard in vitro techniques. In all but one of the arteries tested, ET-3 was significantly less potent than ET-1. In contrast, the potency of ET-3 was very similar to that of ET-1 in all of the veins. The selective ETA receptor antagonist BQ-123 blunted the ET-1 contractions in rabbit carotid artery, but not in saphenous vein. The selective ETB receptor ligand sarafotoxin S6c contracted the rabbit saphenous vein, but not the carotid artery. These data suggest that vascular smooth muscle cells express ETA and ETB receptors. Stimulation of either receptor subtype can result in force development.
Moreland
S
S
Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08540-4000.
McMullen
D M
DM
Delaney
C L
CL
Lee
V G
VG
Hunt
J T
JT
D000818:Animals; D002339:Carotid Arteries / Q000187:drug effects / Q000502:physiology*; D002522:Chlorocebus aethiops; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D016232:Endothelins / Q000378:metabolism / Q000494:pharmacology*; D007083:Iliac Artery / Q000187:drug effects / Q000502:physiology*; D066298:In Vitro Techniques; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000502:physiology*; D009928:Organ Specificity; D011817:Rabbits; D011956:Receptors, Cell Surface / Q000187:drug effects / Q000502:physiology*; D017466:Receptors, Endothelin; D012501:Saphenous Vein / Q000187:drug effects / Q000502:physiology*; D013045:Species Specificity; D014661:Vasoconstriction / Q000187:drug effects / Q000502:physiology*
D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin