Endothelium-dependent relaxation to the B1 kinin receptor agonist des-Arg9-bradykinin in human coronary arteries.
Des-Arg9-bradykinin (des-Arg9-BK) caused endothelium-dependent relaxations in human, isolated coronary arteries which upregulated with in vitro incubation time. Relaxations to des-Arg9-BK were inhibited by the B1 receptor antagonist, des-Arg9-[Leu3]-BK (pK(B), 6.14 +/- 0.11) but were unaffected by the B2 receptor antagonist, Hoe-140. Therefore, this is the first demonstration that human coronary arteries possess endothelial B1 receptors which mediate endothelium-dependent relaxation and appear to be synthesized de novo during the incubation period.
Drummond
G R
GR
Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia.
Cocks
T M
TM
D001920:Bradykinin / Q000031:analogs & derivatives* / Q000494:pharmacology; D003331:Coronary Vessels / Q000187:drug effects* / Q000378:metabolism; D004730:Endothelium, Vascular / Q000187:drug effects* / Q000378:metabolism; D006801:Humans; D066298:In Vitro Techniques; D018002:Receptors, Bradykinin / Q000819:agonists* / Q000096:biosynthesis
D018002:Receptors, Bradykinin; C024626:bradykinin, des-Arg(9)-; C065679:icatibant; D001920:Bradykinin