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

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

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Pharmacy Department, Faculty of Tech. and Engg., The M. S. University of Baroda, Vadodara 390 001, Gujarat, India.


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.

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