Campbell W B, Schmitz J M
Eur J Pharmacol. 1979 Mar 1;54(3):209-16. doi: 10.1016/0014-2999(79)90079-7.
The effects of (7Ile) angiotensin III (AIII) and (1-Sar-8-Ile) angiotensin II (AII) on the pressor and steroidogenic effects of angiotensin were compared in conscious rats. (1-Sar-8-Ile) AII (500 ng/kg/min) equally inhibited the pressor responses of AII, AIII and (des-1-Asp) AI by 99% (P less than 0.0001) while (7-Ile) AIII (500 ng/kg/min) was without effect. The steroidogenic effects of AII, AIII and (des-1-Asp) AI (300 ng/kg/min) were inhibited by (1-Sar-8-Ile) AII by 83%, 69% and 50%, respectively, whereas (7-Ile) AIII inhibited their steroidogenic effects by 35%, 62% and 25%. respectively. In contrast, ACTH or potassium stimulated aldosterone release was not altered by either antagonist. In sodium depleted rats, (7-Ile) AII reduced the elevated serum aldosterone levels by 64% without altering the blood pressure, while (1-Sar-8-Ile) AII lowered the blood pressure without altering the concentration of aldosterone present in the serum. Thus, (7-Ile) AIII is relatively selective in its ability to antagonize the adrenal actions of endogenous and exogenous angiontensins when compared to the pressor actions of these peptides. Furthermore, these angiotensin antagonists appear to be useful as pharmacologic tools in assessing the characteristics of the angiotensin receptors in a particular tissue.
在清醒大鼠中比较了（7-异亮氨酸）血管紧张素III（AIII）和（1-肌氨酸-8-异亮氨酸）血管紧张素II（AII）对血管紧张素升压和类固醇生成作用的影响。（1-肌氨酸-8-异亮氨酸）AII（500 ng/kg/分钟）同等程度地抑制了AII、AIII和（去-1-天冬氨酸）AI的升压反应，抑制率达99%（P<0.0001），而（7-异亮氨酸）AIII（500 ng/kg/分钟）则无此作用。（1-肌氨酸-8-异亮氨酸）AII分别抑制了AII、AIII和（去-1-天冬氨酸）AI（300 ng/kg/分钟）的类固醇生成作用，抑制率分别为83%、69%和50%，而（7-异亮氨酸）AIII分别抑制它们的类固醇生成作用35%、62%和25%。相反，促肾上腺皮质激素或钾刺激的醛固酮释放未被任何一种拮抗剂改变。在缺钠大鼠中，（7-异亮氨酸）AII使升高的血清醛固酮水平降低64%，而血压未改变，而（1-肌氨酸-8-异亮氨酸）AII降低了血压，而血清中醛固酮浓度未改变。因此，与这些肽的升压作用相比，（7-异亮氨酸）AIII在拮抗内源性和外源性血管紧张素的肾上腺作用方面具有相对选择性。此外，这些血管紧张素拮抗剂似乎可用作评估特定组织中血管紧张素受体特性的药理学工具。
