Moore G J, Ko E M
Can J Physiol Pharmacol. 1979 Jul;57(7):763-6. doi: 10.1139/y79-118.
[1-sarcosine, 7-N-methyl-L-alanine, 8-isoleucine]-Angiotensin II and [1-sarcosine, 7-DL-nipecotic acid, 8-isoleucine]-angiotensin II were synthesized by the solid-phase method and purified by cation-exchange chromatography and high-pressure liquid chromatography. In the isolated rat uterus these analogs and less than 0.1% of the myotropic activity of angiotensin II and inhibited angiotensin II with pA2 values of 8.2 and 7.8, respectively. In the rat pressor assay (vagotomized ganglion blocked rat) these analogs had 0.9 and 2.8%, respectively, of the pressor activity of angiotensin II. The results show that the proline residue in position 7 of [Sar1,Ile8]-angiotensin II may be replaced by other secondary amino acids without disrupting interactions at angiotensin II receptors.
[1-肌氨酸，7-N-甲基-L-丙氨酸，8-异亮氨酸]-血管紧张素II和[1-肌氨酸，7-DL-哌啶酸，8-异亮氨酸]-血管紧张素II通过固相法合成，并通过阳离子交换色谱法和高压液相色谱法纯化。在离体大鼠子宫中，这些类似物分别具有小于0.1%的血管紧张素II的促肌活性，并且分别以8.2和7.8的pA2值抑制血管紧张素II。在大鼠升压试验（迷走神经切断神经节阻断大鼠）中，这些类似物分别具有血管紧张素II升压活性的0.9%和2.8%。结果表明，[Sar1，Ile8]-血管紧张素II第7位的脯氨酸残基可以被其他仲氨基酸取代，而不会破坏与血管紧张素II受体的相互作用。
