Biological ActivityHigh affinity, selective ANP clearance receptor (NPR3) antagonist (Ki = 0.45 nM). Exhibits >20,000-fold selectivity for NPR3 over NPR1. Inhibits ANP-stimulated Na+/K+ pump activity in rabbit ventricular cardiomyocytes in vitro. Also blocks proliferation of rodent neonatal cardiomyocytes seen at low ANP concentrations in vitro.
(Modifications: Arg-1 = N2-[4-(2-Naphthoylamino)phenylacetyl], Arg-4 = C-terminal (S)-2-methylbutylamide)
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The discovery of non-basic atrial natriuretic peptide clearance receptor antagonists. Part 1.
Veale et al.
Natriuretic peptides stimulate the cardiac sodium pump via NPR-C-coupled NOS activation.
William et al.
Am.J.Physiol.Cell Physiol., 2008;294:C1067
Differential activation of natriuretic peptide receptors modulates cardiomyocyte proliferation during development.
Becker et al.
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Investigation of NPR3 agonism in blood vessels.