Altinkurt O, Oztürk Y
Department of Pharmacology, Faculty of Pharmacy, University of Ankara, Turkey.
Peptides. 1990 Jan-Feb;11(1):39-44. doi: 10.1016/0196-9781(90)90107-g.
Pharmacological properties of the bradykinin receptors in the isolated rat duodenum were investigated by examining the relaxant and contractile responses to bradykinin and [des-Arg9]-bradykinin, an agonist of B1 receptors. A specific desensitization and de novo formation for B1 receptors were observed. Changes in medium pH caused a decrease in the responses to bradykinin and [des-Arg9]-bradykinin of rat duodenum. Urea incubation in test tube inhibited the responses to bradykinin and [des-Arg9]-bradykinin of rat duodenum, while urea in bathing medium was ineffective. These findings strongly suggested that (a) ionic bonds are important in the interaction between bradykinin and its receptors, and (b) B2 receptors in rat duodenum are different from those in guinea pig ileum.
通过检测对缓激肽和B1受体激动剂[去-精氨酸9]-缓激肽的舒张和收缩反应,研究了分离的大鼠十二指肠中缓激肽受体的药理特性。观察到B1受体存在特异性脱敏和重新形成现象。培养基pH值的变化导致大鼠十二指肠对缓激肽和[去-精氨酸9]-缓激肽的反应降低。试管中尿素孵育抑制了大鼠十二指肠对缓激肽和[去-精氨酸9]-缓激肽的反应,而浴液中的尿素则无效。这些发现强烈表明:(a)离子键在缓激肽与其受体的相互作用中很重要;(b)大鼠十二指肠中的B2受体与豚鼠回肠中的不同。