Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea.
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.
Scherrer
D
D
Laboratoire de Neuroimmunopharmacologie, INSERM U 425, Illkirch, France.
Daeffler
L
L
Trifilieff
A
A
Gies
J P
JP
D000818:Animals; D001667:Binding, Competitive; D065168:Bradykinin Receptor Antagonists; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects; D009281:Naphthalenes / Q000378:metabolism / Q000494:pharmacology*; D009943:Organophosphorus Compounds / Q000378:metabolism / Q000494:pharmacology*; D043782:Receptor, Bradykinin B2; D014132:Trachea / Q000187:drug effects* / Q000378:metabolism / Q000502:physiology
D065168:Bradykinin Receptor Antagonists; D009281:Naphthalenes; D009943:Organophosphorus Compounds; D043782:Receptor, Bradykinin B2; C087374:WIN 64338