Presence of non-selective type of endothelin receptor on vascular endothelium and its linkage to vasodilation.
We studied the role of non-selective type (ETB) of endothelin (ET) receptor in the vasculature, using a ligand specific to the ETB receptor, [Glu9]-sarafotoxin S6b ([Glu9]SRTb). Endothelium-containing rat thoracic aorta possessed specific binding sites for 125I-[Glu9]SRTb, which were almost eliminated by removal of the endothelium, while ET-3-specific binding sites were not detected in the endothelium-intact rat aorta. Only ETB receptor was detected in the membranes from the endothelium of porcine thoracic aorta. [Glu9]SRTb exerted only vasodilation in rat aortic ring. These findings indicate that ETB receptors are located on vascular endothelium and linked to vasodilation.
Takayanagi
R
R
Third Department of Internal Medicine, Faculty of Medicine, Kyushu University, Fukuoka, Japan.
Kitazumi
K
K
Takasaki
C
C
Ohnaka
K
K
Aimoto
S
S
Tasaka
K
K
Ohashi
M
M
Nawata
H
H
D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000502:physiology; D001665:Binding Sites; D001667:Binding, Competitive; D016232:Endothelins / Q000378:metabolism; D004730:Endothelium, Vascular / Q000187:drug effects / Q000378:metabolism / Q000502:physiology*; D051381:Rats; D011956:Receptors, Cell Surface / Q000378:metabolism / Q000502:physiology*; D017466:Receptors, Endothelin; D013552:Swine; D014662:Vasoconstrictor Agents; D014664:Vasodilation / Q000502:physiology*; D014757:Viper Venoms
D016232:Endothelins; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; D014662:Vasoconstrictor Agents; D014757:Viper Venoms; C057354:sarafotoxins s6