Pruneau D, Bélichard P
Centre de Recherche, Laboratoires Fournier S.C.A., Daix, France.
Eur J Pharmacol. 1993 Aug 3;239(1-3):63-7. doi: 10.1016/0014-2999(93)90976-o.
Responses to bradykinin and to the bradykinin B1 receptor agonist des-Arg9-bradykinin were studied in freshly isolated rabbit carotid artery rings and in rings after a 5-h period of incubation. In freshly isolated rings precontracted with noradrenaline, neither bradykinin nor des-Arg9-bradykinin changed the tension whereas acetylcholine relaxed the vessel in a concentration-dependent manner. After incubation, des-Arg9-bradykinin, and to a lesser extent bradykinin, produced an endothelium-dependent relaxation. This response was abolished by endothelium removal, N omega-nitro-L-arginine or cycloheximide but was unaffected by indomethacin. In contrast, the response to acetylcholine was unaffected by cycloheximide and was partially inhibited by N omega-nitro-L-arginine. In addition, the relaxation curve for des-Arg9-bradykinin was markedly shifted (44-fold) by the selective bradykinin B1 receptor antagonist, des-Arg9-[Leu8]bradykinin (3 microM) and was unaffected by the bradykinin B2 receptor antagonist, Hoe 140 (1 microM). We conclude that in vitro incubation of the rabbit carotid artery induced endothelial bradykinin B1 receptors coupled to the release of endothelium-derived nitric oxide.
在新鲜分离的兔颈动脉环以及孵育5小时后的环中，研究了对缓激肽和缓激肽B1受体激动剂去-精氨酸9-缓激肽的反应。在预先用去甲肾上腺素预收缩的新鲜分离环中，缓激肽和去-精氨酸9-缓激肽均未改变张力，而乙酰胆碱以浓度依赖性方式使血管舒张。孵育后，去-精氨酸9-缓激肽以及程度较轻的缓激肽产生了内皮依赖性舒张。这种反应通过去除内皮、Nω-硝基-L-精氨酸或环己酰亚胺而被消除，但不受吲哚美辛影响。相反，对乙酰胆碱的反应不受环己酰亚胺影响，并被Nω-硝基-L-精氨酸部分抑制。此外，选择性缓激肽B1受体拮抗剂去-精氨酸9-[亮氨酸8]缓激肽（3 microM）使去-精氨酸9-缓激肽的舒张曲线明显移位（44倍），并且不受缓激肽B2受体拮抗剂Hoe 140（1 microM）影响。我们得出结论，兔颈动脉的体外孵育诱导了与内皮衍生一氧化氮释放偶联的内皮缓激肽B1受体。
