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The non‐biphenyl‐tetrazole angiotensin AT1 receptor antagonist eprosartan is a unique and robust inverse agonist of the active state of the AT1 receptor

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Conditions such as hypertension and renal allograft rejection are accompanied by chronic, agonist‐independent, signalling by angiotensin II AT1 receptors. The current treatment paradigm for these diseases entails the preferred use… Click to show full abstract

Conditions such as hypertension and renal allograft rejection are accompanied by chronic, agonist‐independent, signalling by angiotensin II AT1 receptors. The current treatment paradigm for these diseases entails the preferred use of inverse agonist AT1 receptor blockers (ARBs). However, variability in the inverse agonist activities of common biphenyl‐tetrazole ARBs for the active state of AT1 receptors often leads to treatment failure. Therefore, characterization of robust inverse agonist ARBs for the active state of AT1 receptors is necessary.

Keywords: at1 receptor; at1; inverse agonist; active state

Journal Title: British Journal of Pharmacology
Year Published: 2018

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