Hui K Y, Holleran E M, Kovacs J
St. John's University, Jamaica, New York.
Int J Pept Protein Res. 1989 Sep;34(3):177-83. doi: 10.1111/j.1399-3011.1989.tb00228.x.
[Ser1]- (32), [D-Ser1]-(29), [Ser1, Leu8]-(31), and [D-Ser1, Leu8] angiotensin II (30) were synthesized by a repetitive method in solution using new protected amino acid 2,3,5,6- tetrafluorophenyl active esters. 32 and 29 were agonists, and 31 and 30 were specific antagonists to angiotensin II (AII) receptors determined by the rabbit aortic strip (RAS) and rat blood pressure (RBP) assays. It was found that the hydroxymethyl side chains of serine and D-serine in position-1 has an important influence on the agonistic activity of the analogues. The pressor activities of 32 and 29 were 129 and 314%, respectively, as potent as AII. On the other hand, 31 and 30 were effective in antagonizing the AII-induced contraction of RAS and rise in RBP.
通过在溶液中使用新型保护氨基酸2,3,5,6 - 四氟苯基活性酯的重复方法合成了[Ser1] - (32)、[D - Ser1] - (29)、[Ser1, Leu8] - (31)和[D - Ser1, Leu8]血管紧张素II (30)。通过兔主动脉条(RAS)和大鼠血压(RBP)测定法确定，32和29是激动剂，31和30是血管紧张素II (AII)受体的特异性拮抗剂。发现1位丝氨酸和D - 丝氨酸的羟甲基侧链对类似物的激动活性有重要影响。32和29的升压活性分别为AII的129%和314%。另一方面，31和30能有效拮抗AII诱导的RAS收缩和RBP升高。
