非肽类缓激肽B2受体拮抗剂WIN 64338对豚鼠气管的作用。
Effects of WIN 64338, a nonpeptide bradykinin B2 receptor antagonist, on guinea-pig trachea.
作者信息
Scherrer D, Daeffler L, Trifilieff A, Gies J P
机构信息
Laboratoire de Neuroimmunopharmacologie, INSERM U 425, Illkirch, France.
出版信息
Br J Pharmacol. 1995 Aug;115(7):1127-8. doi: 10.1111/j.1476-5381.1995.tb15013.x.
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.
摘要
我们研究了非肽类缓激肽受体拮抗剂[[4-[[2-[[双(环己基氨基)亚甲基]氨基]-3-(2-萘基)-1-氧代丙基]氨基]苯基]-三丁基氯化铵，单盐酸盐(WIN 64338)对豚鼠气管[3H]-缓激肽结合及缓激肽诱导收缩的影响。这种非肽类缓激肽受体拮抗剂以纳摩尔范围的亲和力抑制[3H]-缓激肽结合，Ki = 50.9±19 nM，并以非竞争性方式抑制缓激肽诱导的收缩，KB值为6.43×10(-8)±2.34×10(-8) M。
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