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缓激肽和胰激肽的受体。

Receptors for bradykinin and kallidin.

作者信息

Drouin J N, St-Pierre S A, Regoli D

出版信息

Can J Physiol Pharmacol. 1979 Apr;57(4):375-9. doi: 10.1139/y79-056.

Abstract

In order to establish if bradykinin (BK) and Lys-bradykinin (Lys-BK), alias kallidin, act on the same or on different receptors, experiments were performed on strips of cat terminal ileum and of rabbit aorta. The first preparation contains receptor B2 and the second has the newly identified receptor B1. The criterion used for establishing the identity of receptors for BK and Lys-BK in the cat ileum (receptor B2) was desensitization, while for the rabbit aorta (receptor B1) we measured the apparent affinity (pA2 value) of a competitive and specific inhibitor of BK, [Leu-OMe3,des-Arg9]-BK. Since cat ileum desensitized with BK or Lys-BK shows a significant decrease or a complete disappearance of the response to the other agent, while maintaining full sensitivity for histamine, and since the pA2 values of [Leu-OMe8,des-Arg9]-BK against BK and Lys-BK are identical in the rabbit aorta, we conclude that the two kinins act on the same types of receptors.

摘要

为了确定缓激肽(BK)和赖氨酸缓激肽(Lys - BK,又名胰激肽)作用于相同还是不同的受体,我们在猫的回肠末端条和兔的主动脉条上进行了实验。第一种标本含有B2受体,第二种标本含有新发现的B1受体。用于确定猫回肠中BK和Lys - BK受体(B2受体)一致性的标准是脱敏,而对于兔主动脉(B1受体),我们测量了BK的竞争性特异性抑制剂[亮氨酸 - 甲酯3,去精氨酸9] - BK的表观亲和力(pA2值)。由于用BK或Lys - BK脱敏的猫回肠对另一种药物的反应显著降低或完全消失,而对组胺仍保持完全敏感性,并且由于[亮氨酸 - 甲酯8,去精氨酸9] - BK对BK和Lys - BK的pA2值在兔主动脉中是相同的,我们得出结论,这两种激肽作用于相同类型的受体。

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