Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists—A perspective

Hypertension is a major risk factor for human morbidity and mortality through its effects on target organs like heart, brain and kidneys. More intensive treatment for the effective control of blood pressure significantly reduces the morbidity and mortality. The renin angiotensin system (RAS) is a coordinated hormonal cascade of major clinical importance in the regulation of blood pressure. The principal effector peptide of RAS is angiotensin II, which acts by binding to one of the two major angiotensin II receptors AT1 and AT2. Angiotensin II through AT1 receptor mediates vast majority of biologically detrimental actions. Nonpeptidic angiotensin II (AT1) antagonists are the most specific means to block the renin angiotensin enzymatic cascade available presently. Majority of AT1 antagonists are based on modifications of losartan structure, the first clinically used AT1 antagonist. In this review, a comprehensive presentation of the literature on AT1 receptor antagonists has been given.

Figure optionsDownload as PowerPoint slide