Ueno A, Oh-ishi S
Department of Pharmacology, Kitasato University School of Pharmaceutical Sciences, Tokyo, Japan.
Nihon Yakurigaku Zasshi. 1997 Oct;110 Suppl 1:104P-107P. doi: 10.1254/fpj.110.supplement_104.
We found the time-dependent induction of the systemic hypotensive response to des-Arg9-bradykinin and the contractile response of ileum of rats to des-Arg9-bradykinin. Both induced responses to des-Arg9-bradykinin were inhibited by treatment with a B1 receptor competitive antagonist, while the responses to bradykinin was constant throughout the experiment and was not influenced by the B1 antagonist, suggesting that these responses occur via a B1 receptor. The potencies of des-Arg9-bradykinin in these responses were comparable to those of bradykinin at a molar base. The other characteristics of this phenomenon is that several hours were required to the induction of these responses. In a case of hypotensive response, intravenous LPS pretreatment was necessary, but not for the induction of contraction in ileum preparation. Treatment with actinomycin D or cycloheximide throughout the experiment suppressed the induction of the contractile response to des-Arg9-bradykinin. The expression of B1 receptor gene was also confirmed by a RT-PCR method. Therefore, we concluded that these responses to des-Arg9-bradykinin occurred via a B1 receptor, which could be newly generated time-dependently.
我们发现了大鼠对去精氨酸9-缓激肽的全身降压反应以及回肠对去精氨酸9-缓激肽的收缩反应的时间依赖性诱导。用B1受体竞争性拮抗剂处理可抑制对去精氨酸9-缓激肽的这两种诱导反应,而对缓激肽的反应在整个实验过程中保持恒定,且不受B1拮抗剂影响,这表明这些反应是通过B1受体发生的。去精氨酸9-缓激肽在这些反应中的效力与缓激肽在摩尔基础上的效力相当。这种现象的另一个特点是诱导这些反应需要几个小时。在降压反应的情况下,静脉注射LPS预处理是必要的,但对于回肠制备中的收缩诱导则不是必需的。在整个实验过程中用放线菌素D或环己酰亚胺处理可抑制对去精氨酸9-缓激肽的收缩反应诱导。B1受体基因的表达也通过RT-PCR方法得到证实。因此,我们得出结论,对去精氨酸9-缓激肽的这些反应是通过B1受体发生的,该受体可能随时间依赖性地新生成。