Paiva A C, Paiva T B, Miyamoto M E, Nakaie C R
Mayo Clin Proc. 1977 Jul;52(7):427-9.
The role of Ca++ in the stimulus-contraction coupling of the response of the isolated rabbit aorta to angiotensin II was investigated. Angiotensin was found to have lower intrinsic activity than epinephrine and to be more sensitive to acute exposure of the organ to Ca++-free medium. Two minutes after removal of Ca++, the maximal responses to angiotensin and epinephrine were reduced by 40% +/- 8% and 7% +/- 5%, respectively. Further loss of response for the two agonists followed parallel time courses. In another series of experiments, angiotensin tachyphylaxis was obtained in the rabbit aorta by administration of either [1-sarcosine]angiotensin or betainyl-angiotensin. The intrinsic activity of [1-sarcosine]angiotensin was lower than that of angiotensin and was not affected by removal of Ca++. It is concluded that the low intrinsic activity and the tachyphylaxis may be dependent on a strong binding of the molecule's positively charged N-terminus to sites responsible for release of Ca++ into the cell.
研究了钙离子(Ca++)在离体兔主动脉对血管紧张素II反应的刺激-收缩偶联中的作用。发现血管紧张素的内在活性低于肾上腺素,并且对器官急性暴露于无钙培养基更为敏感。去除钙离子两分钟后,对血管紧张素和肾上腺素的最大反应分别降低了40%±8%和7%±5%。两种激动剂反应的进一步丧失遵循平行的时间进程。在另一系列实验中,通过给予[1-肌氨酸]血管紧张素或甜菜碱血管紧张素,在兔主动脉中获得了血管紧张素快速耐受性。[1-肌氨酸]血管紧张素的内在活性低于血管紧张素,并且不受去除钙离子的影响。得出的结论是,低内在活性和快速耐受性可能取决于分子带正电荷的N端与负责将钙离子释放到细胞中的位点的强结合。