ang-1-7 receptor

AVE 0991 competes for high-affinity binding of [125I]-Ang-(1-7) to bovine aortic endothelial cell membranes, with IC50 of 21±35 nM. AVE 0991 sodium salt is a nonpeptide and orally active Ang-(1-7) receptor Mas agonist.

Alamandine can be formed from angiotensin A by action of ACE-2 or directly from angiotensin-(1-7) by decarboxylation of its aspartate residue. The angiotensin A analog produces effects resembling those of Ang II (1-7). However, it acts independently of the two known vasodilators receptors of the RAS (Mas and angiotensin II type 2). To produce its effects, alamandine binds to the Mas-related receptor, MrgD. A novel orally active formulation of alamandine produced a long-term antihypertensive effect in spontaneously hypertensive rats and cardioprotective effects. These novel findings will be helpful for developing a new understanding of the RAS, a key regulator of blood pressure and fluid balance. The heptapeptide could serve as a model peptide, e.g. in the development and evaluation of analytical methods.

Angiotensin (1-7) (ASP-ARG-VAL-TYR-ILE-HIS-PRO) 是肾素-血管紧张素系统中的内源性七肽。Angiotensin 1-7在心肌细胞中具有抗炎和抗纤维化活性，因此具有心脏保护作用。它能抑制血管紧张素转换酶和释放一氧化氮，是激肽诱导的血管舒张的局部协同调节剂。它阻断 Ang II 诱导的平滑肌细胞增殖和肥大，并显示对内皮的抗血管生成和生长抑制作用。它显示出抗炎活性。

AVE 0991 是血管紧张素-(1-7) [Ang-(1-7)] 的非肽类似物，是一种具有口服活性的 Mas 激动剂，对 [125I]-Ang-(1-7) 结合到牛主动脉内皮细胞膜有抑制作用，通过增强自噬来抑制星形胶质细胞介导的阿尔茨海默病神经炎症。