Kwok Y G, Moore G J
Eur J Pharmacol. 1985 Sep 10;115(1):53-8. doi: 10.1016/0014-2999(85)90583-7.
The isolated rat uterus and rabbit aorta were photolabelled with [Azidobenzoic acid 1, isoleucine8]angiotensin II ([AB', Ile8]ANG II) and dose-response curves to angiotensins II and III were determined before and after the irreversible labelling procedure. The data obtained were used to calculate affinities, efficacies and 'spare' receptors for angiotensins II and III. In the rat uterus angiotension II was the higher affinity ligand, whereas in the rabbit aorta angiotensins II and III had similar affinities. 'Spare' receptors were present for both ligands in both tissues. In the rat uterus ANG II and ANG III had similar efficacies, whereas in the rabbit aorta ANG II was the more efficacious ligand. Angiotensin receptors in the rabbit aorta, rat uterus, and rat portal vein appear to be substantially different from one another, and point to the possibility of different functional roles for angiotensins II and III in different smooth muscle tissues. For the vascular tissues, tachyphylaxis to angiotensin was more marked after irreversible labelling than before, suggesting that the mechanism of angiotensin tachyphylaxis is receptor deactivation.
将离体大鼠子宫和兔主动脉用[叠氮苯甲酸1,异亮氨酸8]血管紧张素II([AB',Ile8]ANG II)进行光标记,并在不可逆标记程序前后测定对血管紧张素II和III的剂量反应曲线。所获得的数据用于计算血管紧张素II和III的亲和力、效能和“备用”受体。在大鼠子宫中,血管紧张素II是亲和力较高的配体,而在兔主动脉中,血管紧张素II和III具有相似的亲和力。两种组织中两种配体均存在“备用”受体。在大鼠子宫中,ANG II和ANG III具有相似的效能,而在兔主动脉中,ANG II是效能更高的配体。兔主动脉、大鼠子宫和大鼠门静脉中的血管紧张素受体似乎彼此有很大差异,这表明血管紧张素II和III在不同平滑肌组织中可能具有不同的功能作用。对于血管组织,不可逆标记后对血管紧张素的快速耐受性比标记前更明显,提示血管紧张素快速耐受性的机制是受体失活。