Autocrine receptors for endothelins in the primary culture of endothelial cells of human umbilical vein.
Human umbilical vein endothelial cells (HUVECs) in primary culture produced and secreted endothelin 1 (ET-1) actively. Specific binding of [125I]ET-1 to these cells was not detectable because of the saturation of ET receptors with endogenously produced ET-1. However, addition of phosphoramidon, an inhibitor of ET-converting enzyme, to the medium reduced the production of ET-1 and thus the receptors on HUVECs were made available for exogenously added [125I]ET-1. Binding studies using phosphoramidon-treated HUVECs indicated the existence of a non-isopeptide-selective type (ETB) of ET receptor with a Kd of 17 pM. This receptor is thought to be involved in ET-induced vasodilation in an autocrine manner in vivo.
Fujitani
Y
Y
International Research Laboratories, CIBA-GEIGY Limited, Takarazuka, Japan.
Oda
K
K
Takimoto
M
M
Inui
T
T
Okada
T
T
Urade
Y
Y
D001665:Binding Sites / Q000187:drug effects; D002452:Cell Count / Q000187:drug effects; D002478:Cells, Cultured; D016232:Endothelins / Q000096:biosynthesis / Q000187:drug effects / Q000378:metabolism*; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D006020:Glycopeptides / Q000494:pharmacology; D006801:Humans; D007700:Kinetics; D011956:Receptors, Cell Surface / Q000032:analysis* / Q000187:drug effects; D017466:Receptors, Endothelin; D014471:Umbilical Veins
D016232:Endothelins; D006020:Glycopeptides; D011956:Receptors, Cell Surface; D017466:Receptors, Endothelin; C008890:phosphoramidon