新型高效缓激肽受体拮抗剂在豚鼠气管中的比较作用
Comparative action of new highly potent bradykinin receptor antagonists in the guinea-pig trachea.
作者信息
Trifilieff A, Amrani Y, Landry Y, Gies J P
机构信息
Laboratoire de Neuroimmunopharmacologie, INSERM CJF-9105, Université Louis Pasteur Strasbourg I, Faculté de Pharmacie, Illkirch, France.
出版信息
Eur J Pharmacol. 1993 Aug 3;239(1-3):227-9. doi: 10.1016/0014-2999(93)91000-d.
We investigated the effect of two new bradykinin receptor antagonists, D-Arg0[Hyp3,D-HypE(trans-propyl)7,Oic8]bradykinin (NPC 17731) and D-Arg0[Hyp3,D-HypE(trans-thiophenyl)7,Oic8]bradykinin (NPC 17761) on [3H]bradykinin binding and on bradykinin-induced contraction of the guinea-pig trachea. Both of these compounds inhibited [3H]bradykinin binding with an affinity similar to that of unlabelled bradykinin. NPC 17731 inhibited bradykinin-induced contraction in a non-competitive manner, whereas NPC 17761 showed competitive antagonism. Therefore, NPC 17761 could contribute to the investigation of the bradykinin receptors in guinea-pig airways.
我们研究了两种新型缓激肽受体拮抗剂，D-Arg0[Hyp3,D-HypE（反式丙基）7,Oic8]缓激肽（NPC 17731）和D-Arg0[Hyp3,D-HypE（反式噻吩基）7,Oic8]缓激肽（NPC 17761）对[3H]缓激肽结合以及对豚鼠气管缓激肽诱导收缩的影响。这两种化合物均以与未标记缓激肽相似的亲和力抑制[3H]缓激肽结合。NPC 17731以非竞争性方式抑制缓激肽诱导的收缩，而NPC 17761表现出竞争性拮抗作用。因此，NPC 17761有助于对豚鼠气道中缓激肽受体的研究。
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