Muñoz-Ramírez H, Khosla M C, Hall M M, Bumpus F M, Khairallah P A
Res Commun Chem Pathol Pharmacol. 1976 Apr;13(4):649-63.
The capacity of (1-Sarcosine, 8-Threonine) angiotensin II to block the contractile and pressor effects of exogenous and endogenous angiotensin II was examined. In isolated rabbit aorta, the pA2 value (from pA2 plots) for the analog was 8.75 +/- 0.11. Both the maximum response and the slope of the dose-response curve to angiotensin II were unchanged by the analog. In ganglion-blocked vagotomized rats, infusion of the analog produced a dose-dependent blockage of the angiotensin II pressor effect. In these rats, the analog displayed less agonistic activity than that of (1-Sarcosine, 8-Isoleucine) and (1-Sarcosine, 8-Alanine) angiotensin II. In two-kidney hypertensive rats, the angiotensin II antagonist significantly reduced the arterial blood pressure. The results indicate that (1-Sar, 8-Thr) angiotensin II is a potent antagonist of angiotensin II with less inherent agonistic activity than previously reported analogs.
研究了（1-肌氨酸，8-苏氨酸）血管紧张素II阻断外源性和内源性血管紧张素II的收缩和升压作用的能力。在离体兔主动脉中，该类似物的pA2值（根据pA2图）为8.75±0.11。该类似物对血管紧张素II的最大反应和剂量反应曲线的斜率均未改变。在神经节阻断的迷走神经切断大鼠中，输注该类似物会产生剂量依赖性的血管紧张素II升压作用阻断。在这些大鼠中，该类似物的激动活性低于（1-肌氨酸，8-异亮氨酸）和（1-肌氨酸，8-丙氨酸）血管紧张素II。在二肾性高血压大鼠中，血管紧张素II拮抗剂显著降低了动脉血压。结果表明，（1-肌氨酸，8-苏氨酸）血管紧张素II是一种有效的血管紧张素II拮抗剂，其内在激动活性低于先前报道的类似物。
