Comparative action of new highly potent bradykinin receptor antagonists in the guinea-pig trachea.
We investigated the effect of two new bradykinin receptor antagonists, D-Arg0[Hyp3,D-HypE(trans-propyl)7,Oic8]bradykinin (NPC 17731) and D-Arg0[Hyp3,D-HypE(trans-thiophenyl)7,Oic8]bradykinin (NPC 17761) on [3H]bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. Both of these compounds inhibited [3H]bradykinin binding with an affinity similar to that of unlabelled bradykinin. NPC 17731 inhibited bradykinin-induced contraction in a non-competitive manner, whereas NPC 17761 showed competitive antagonism. Therefore, NPC 17761 could contribute to the investigation of the bradykinin receptors in guinea-pig airways.
Trifilieff
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A
Laboratoire de Neuroimmunopharmacologie, INSERM CJF-9105, Université Louis Pasteur Strasbourg I, Faculté de Pharmacie, Illkirch, France.
Amrani
Y
Y
Landry
Y
Y
Gies
J P
JP
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001920:Bradykinin / Q000378:metabolism / Q000494:pharmacology / Q000031:analogs & derivatives; D065168:Bradykinin Receptor Antagonists; D004305:Dose-Response Relationship, Drug; D006168:Guinea Pigs; D066298:In Vitro Techniques; D007705:Kinins / Q000037:antagonists & inhibitors*; D009119:Muscle Contraction / Q000187:drug effects; D009130:Muscle, Smooth / Q000187:drug effects*; D009842:Oligopeptides / Q000494:pharmacology*; D018002:Receptors, Bradykinin / Q000378:metabolism; D014132:Trachea / Q000187:drug effects* / Q000378:metabolism
D065168:Bradykinin Receptor Antagonists; D007705:Kinins; D009842:Oligopeptides; D018002:Receptors, Bradykinin; C071327:NPC 17731; C083947:NPC 17761; D001920:Bradykinin