Endothelin-A receptors mediate contraction in human cerebral, meningeal and temporal arteries.
Endothelin-1 (ET-1), an endothelium-derived vasoconstrictor peptide, produced strong contractions in human cerebral, meningeal and temporal arteries. The isopeptides ET-2 and ET-3 also showed potent constrictor activity; however, ET-3 was less potent. The selective ETA receptor antagonist FR 139317 mediated a shift to the right of the concentration-response curve of ET-1. These results suggest that the powerful constriction elicited by the endothelin-isopeptides in cerebral, meningeal and temporal arteries is mediated through ETA receptors.
Department of Internal Medicine, University Hospital of Lund, Sweden.
M
M
Adner
I
I
Jansen
L
L
Edvinsson
D001381:Azepines / Q000494:pharmacology; D002536:Cerebral Arteries / Q000187:drug effects; D065128:Endothelin Receptor Antagonists; D016232:Endothelins / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D007211:Indoles / Q000494:pharmacology; D008576:Meningeal Arteries / Q000187:drug effects; D009119:Muscle Contraction / Q000187:drug effects; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D013699:Temporal Arteries / Q000187:drug effects; D014661:Vasoconstriction / Q000187:drug effects*
D001381:Azepines; D065128:Endothelin Receptor Antagonists; D016232:Endothelins; D007211:Indoles; C079574:FR 139317