Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea.
Fiche publication
Date publication
août 1995
Journal
British journal of pharmacology
Auteurs
Membres identifiés du Cancéropôle Est :
Pr GIES Jean-Pierre, Dr DAEFFLER Laurent
Tous les auteurs :
Scherrer D, Daeffler L, Trifilieff A, Gies JP
Lien Pubmed
Résumé
We investigated the effect of the nonpeptide bradykinin receptor antagonist, [[4-[[2-[[bis(cyclohexylamino)methylene] amino]-3-(2-naphthalenyl) 1-oxopropyl]amino]-phenyl]-tributyl, chloride, monohydrochloride (WIN 64338), on [3H]-bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. This non peptide bradykinin receptor antagonist inhibited [3H]-bradykinin binding with a nanomolar range of affinity, Ki = 50.9 +/- 19 nM and inhibited bradykinin-induced contraction in a non-competitive manner with a KB value of 6.43 10(-8) +/- 2.34 10(-8) M.
Mots clés
Animals, Binding, Competitive, Bradykinin Receptor Antagonists, Guinea Pigs, In Vitro Techniques, Muscle Contraction, drug effects, Naphthalenes, metabolism, Organophosphorus Compounds, metabolism, Receptor, Bradykinin B2, Trachea, drug effects
Référence
Br. J. Pharmacol.. 1995 Aug;115(7):1127-8