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Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea
D Scherrer1, L Daeffler, A Trifilieff
1Laboratoire de Neuroimmunopharmacologie, INSERM U 425, Illkirch, France.
British Journal of Pharmacology
|August 1, 1995
Abstract:
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.