Non-selectivity of new bradykinin antagonists for B1 receptors.
Two new B1 receptor antagonists, [Hyp3,Thi5,DTic7,Oic8]desArg9-BK and DArg[Hyp3,Thi5,DTic7,Oic8]desArg9-BK were tested in vitro on the rabbit jugular vein and the guinea pig ileum (preparations containing B2 receptors) and on the rabbit aorta (preparation containing B1 receptors) for pharmacological characterization. The results indicate that both compounds are antagonists on both B1 and B2 receptors, are competitive and discriminate between B2A and B2B receptor subtypes.
Rhaleb
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Department of Pharmacology, Medical School, University of Sherbrooke, Québec, Canada.
Gobeil
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Regoli
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D000595:Amino Acid Sequence; D000818:Animals; D001011:Aorta / Q000187:drug effects / Q000648:ultrastructure; D001667:Binding, Competitive; D001920:Bradykinin / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000187:drug effects / Q000648:ultrastructure; D066298:In Vitro Techniques; D007601:Jugular Veins / Q000187:drug effects / Q000648:ultrastructure; D007700:Kinetics; D008969:Molecular Sequence Data; D009130:Muscle, Smooth / Q000187:drug effects / Q000648:ultrastructure; D009131:Muscle, Smooth, Vascular / Q000187:drug effects / Q000648:ultrastructure; D009842:Oligopeptides / Q000494:pharmacology*; D011817:Rabbits; D018002:Receptors, Bradykinin; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors* / Q000145:classification; D044005:Tetrahydroisoquinolines
D009842:Oligopeptides; D018002:Receptors, Bradykinin; D017981:Receptors, Neurotransmitter; D044005:Tetrahydroisoquinolines; C078665:HOE 140, desArg(10)-; C076640:bradykinin, Hyp(3)-Thi(5)-Tic(7)-Oic(8)-desArg(9)-; C024626:bradykinin, des-Arg(9)-; C051090:bradykinin, Leu(8)-des-Arg(9)-; C065679:icatibant; D001920:Bradykinin