EFFECTS OF WIN-64338, A NONPEPTIDE BRADYKININ B-2 RECEPTOR ANTAGONIST, ON GUINEA-PIG TRACHEA

We investigated the effect of the nonpeptide bradykinin receptor antag onist, [[4-[[2-[[bis(cyclohexylamino)methylene] amino]-3-(2-naphthalen yl) 1-oxopropyl]amino]-phenyl]-tributyl, chloride, monohydrochloride ( WIN 64338), on [H-3]-bradykinin binding and on bradykinin-induced cont raction of the guinea-pig trachea. This non peptide bradykinin recepto r antagonist inhibited [H-3]-bradykinin binding with a nanomolar range of affinity, K-i = 50.9 +/- 19 nM and inhibited bradykinin-induced co ntraction in anon-competitive manner with a K-B value of 6.43 10(-8) /- 2.34 10(-8) M.