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• W23967959 abstract "The angiotensin II (AngII) type 1 (AT₁) receptor is a seven-transmembrane G-protein-coupled receptor that plays a regulatory role in the physiological and pathological processes of the cardiovascular system. AT₁ receptor inherently shows constitutive activity even in the absence of AngII, and it is activated not only by AngII but also by AngII-independent mechanisms. Especially, mechanical stress induces cardiac hypertrophy through activation of AT₁ receptor without the involvement of AngII. These AngII-independent activities of AT₁ receptor can be inhibited by inverse agonists, but not by neutral antagonists. In this chapter, we describe the methods used for biochemical assessment of inverse agonism of a ligand for AT₁ receptor. Their applications will improve our understanding of receptor activation and inactivation at a molecular level, and contribute to the development of AT₁ receptor blockers possessing superior therapeutic efficacy in cardiovascular diseases." @default.
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• W23967959 date "2010-01-01" @default.
• W23967959 modified "2023-09-25" @default.
• W23967959 title "Assessment of Inverse Agonism for the Angiotensin II Type 1 Receptor" @default.
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• W23967959 doi "https://doi.org/10.1016/b978-0-12-381296-4.00002-6" @default.
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