Biological Activity
1h-1-ethyl candesartan cilexetil, which is a process-related impurity commonly found in the bulk synthesis of candesartan cilexetil, is a potent, long-acting, and selective angiotensin ii type 1 receptor (at1) antagonist.angiotensin ii is a peptide that is mainly generated by the angiotensin converting enzyme and chymase, which plays a vital role in regulating blood pressure and sodium homeostasis via specific receptors including at1[1]. at1, localized in the kidney, heart, brain, adrenal gland, adipocytes, vascular smooth muscle cells, platelets, and placenta, is a major component of the renin-angiotensin system. furthermore, at1 mediates the classical biological actions of angiotensin ii. also, at1 has seven helical transmembrane domains, which is the characteristic of the superfamily of g-protein-coupled receptors. carboxyl-terminal region structure of at1 plays important roles in receptor internalization, desensitization and phosphorylation [2].
References
[1]. otsuka, m. reduction of bleomycin induced lung fibrosis by candesartan cilexetil, an angiotensin ii type 1 receptor antagonist. thorax. 2004; 59(1): 31-38.
[2]. guo, d., sun, y., hamet, p., & inagami, t. the angiotensin ii type 1 receptor and receptor-associated proteins. cell research. 2001; 11(3): 165-180.