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NPR-A, also known as Natriuretic Peptide Receptor A or guanylyl cyclase-A (GC-A), is a transmembrane receptor that plays a central role in cardiovascular and renal regulation. It is primarily activated by two endogenous ligands: atrial natriuretic peptide (ANP) and B-type natriuretic peptide (BNP). Upon ligand binding, the receptor dimerizes, activating its guanylyl cyclase activity, which converts GTP to cGMP, leading to vasodilation, natriuresis, diuresis, and cardioprotection. Deficiency or dysfunction in NPR-A signaling is associated with hypertension, heart failure, and metabolic syndrome.
Agonists enhance beneficial effects on blood pressure regulation; antagonists may be used where excessive NP signaling contributes to pathology. Binding of ANP or BNP triggers cGMP production and PKG activation, leading to vasodilation, natriuresis, and diuresis.
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