Moore G J, Oudeman E M, Ko D, Nystrom D M
J Med Chem. 1979 Sep;22(9):1147-9. doi: 10.1021/jm00195a032.
Analogues of the type [1-sarcosine,7-sarcosine, 8-X]angiotensin II, where X = isoleucine, leucine, alanine, methionine, O-methylthreonine, or DL-alloisoleucine, were synthesized by the solid-phase method and purified by partition chromatography, cation-exchange chromatography, and high-pressure liquid chromatography. In the isolated rat uterus, these analogues had activities of less than 0.1, less than 0.1, less than 0.1, less than 0.1, less than 0.1, and 0.7%, respectively, of the hyotropic activity of angiotensin II and inhibited the contractile response to angiotensin II with pA2 values of 8.1, 7.2, 6.7, 7.7, 7.4, and 8.4, respectively. In the vagotomized ganglion blocked rat, the analogues had 0.7, 0.21, 0.06, 0.72, 0.13, and 12.5%, respectively, of the pressor activity of angiotensin II.
通过固相法合成了[1-肌氨酸，7-肌氨酸，8-X]血管紧张素II类型的类似物，其中X =异亮氨酸、亮氨酸、丙氨酸、甲硫氨酸、O-甲基苏氨酸或DL-别异亮氨酸，并通过分配色谱法、阳离子交换色谱法和高压液相色谱法进行纯化。在离体大鼠子宫中，这些类似物的促生长活性分别为血管紧张素II的不到0.1%、不到0.1%、不到0.1%、不到0.1%、不到0.1%和0.7%，并以pA2值分别为8.1、7.2、6.7、7.7、7.4和8.4抑制对血管紧张素II的收缩反应。在切断迷走神经节阻断的大鼠中，这些类似物的升压活性分别为血管紧张素II的0.7%、0.21%、0.06%、0.72%、0.13%和12.5%。
