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Mechanism of action of angiotensin-receptor blocking agents

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Abstract

Angiotensin II is the most active hormone of the reninangiotensin system. In humans, two angiotensin receptors have been identified: AT1 and AT2. In adults, most of the effects of angiotensin II are mediated by the AT1 receptor; the function of the AT2 receptor is not yet well established. Angiotensin II has both systemic and local paracrine effects. Increased activity of angiotensin II and stimulation of the AT1 receptor have been linked to the development of several cardiovascular and renal diseases, including hypertension, heart failure, left ventricular hypertrophy, and diabetic nephropathy. Over the past two decades, angiotensin-converting enzymes have been used to manage these diseases. However, the side effects and less-thanmaximum therapeutic effects of angiotensin-converting enzyme inhibitors, particularly in the decrease of mortality associated with congestive heart failure, have led to the development of AT1-receptor blockers.

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Siragy, H.M., Bedigian, M. Mechanism of action of angiotensin-receptor blocking agents. Current Science Inc 1, 289–295 (1999). https://doi.org/10.1007/s11906-999-0036-3

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