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

被引：10

作者：

SCHERRER, D

DAEFFLER, L

TRIFILIEFF, A

GIES, JP

机构：

来源：

BRITISH JOURNAL OF PHARMACOLOGY | 1995年 / 115卷 / 07期

关键词：

BRADYKININ; NONPEPTIDE BRADYKININ RECEPTOR ANTAGONIST; TRACHEA; BRADYKININ BINDING;

D O I：

10.1111/j.1476-5381.1995.tb15013.x

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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 [H-3]-bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. This non peptide bradykinin receptor antagonist inhibited [H-3]-bradykinin binding with a nanomolar range of affinity, K-i = 50.9 +/- 19 nM and inhibited bradykinin-induced contraction in anon-competitive manner with a K-B value of 6.43 10(-8) +/- 2.34 10(-8) M.

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页码：1127 / 1128

页数：2

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