Relaxation of human temporal artery by endothelin ETB receptors.
Endothelin receptors have been characterized in human temporal artery by molecular biological methods and in vitro pharmacology. Reverse transcriptase-polymerase chain reaction was used to detect mRNA encoding ETA and ETB receptors in normal and endothelium-denuded arteries. Vasomotor response experiments with a specific ETA antagonist (FR 139317) suggested the presence of ETA subtypes. Marked ETB-mediated relaxation was obtained with ET-3 when ETA activity was blocked in precontracted arteries. Relaxation was significantly reduced by bosentan, indomethacin, and a nitric oxide synthase inhibitor. It may be speculated that the relaxant activity is mediated through ETB1 receptors.
Lucas
G A
GA
Department of Neurology, University Hospital of Trondheim, Norway.
White
L R
LR
Juul
R
R
Cappelen
J
J
Aasly
J
J
Edvinsson
L
L
D001381:Azepines / Q000494:pharmacology; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000037:antagonists & inhibitors / Q000494:pharmacology; D004730:Endothelium, Vascular / Q000502:physiology; D006801:Humans; D007211:Indoles / Q000494:pharmacology; D010446:Peptide Fragments / Q000494:pharmacology; D017466:Receptors, Endothelin / Q000502:physiology*; D013699:Temporal Arteries / Q000502:physiology*; D014664:Vasodilation / Q000187:drug effects / Q000502:physiology
D001381:Azepines; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D007211:Indoles; D010446:Peptide Fragments; D017466:Receptors, Endothelin; C074308:sovateltide; C079574:FR 139317