Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.

Article Details


Naik P, Murumkar P, Giridhar R, Yadav MR

Angiotensin II receptor type 1 (AT1) selective nonpeptidic antagonists--a perspective.

Bioorg Med Chem. 2010 Dec 15;18(24):8418-56. doi: 10.1016/j.bmc.2010.10.043. Epub 2010 Nov 9.

PubMed ID
21071232 [ View in PubMed

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 AT(1) and AT(2). Angiotensin II through AT(1) receptor mediates vast majority of biologically detrimental actions. Nonpeptidic angiotensin II (AT(1)) antagonists are the most specific means to block the renin angiotensin enzymatic cascade available presently. Majority of AT(1) antagonists are based on modifications of losartan structure, the first clinically used AT(1) antagonist. In this review, a comprehensive presentation of the literature on AT(1) receptor antagonists has been given.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Candesartan cilexetilType-1 angiotensin II receptorIC 50 (nM)110N/AN/ADetails
ForasartanType-1 angiotensin II receptorIC 50 (nM)6.9N/AN/ADetails
IrbesartanType-1 angiotensin II receptorIC 50 (nM)20.8N/AN/ADetails