Apelin, the Novel Endogenous Ligand of the Orphan Receptor APJ, Regulates Cardiac Contractility
Szokodi I, Tavi P, Földes G, Voutilainen-Myllylä S, Ilves M, Tokola H, Pikkarainen S, Piuhola J, Rysä J, Tóth M, Ruskoaho H
Circulation Research · Vol. 91(5) · pp. 434–440 · 2002
Characterization of apelin-13 as a potent positive inotrope that improves cardiac contractility via the APJ receptor. Establishes the apelin/APJ system as a novel cardioprotective pathway with therapeutic potential in heart failure.
Key Findings
Apelin-13 is the most potent endogenous positive inotrope identified to date
Increases cardiac contractility via APJ receptor-mediated PKC and PI3K activation
Reduces cardiac afterload via vasodilation while increasing contractility
APJ receptor expression upregulated in failing human hearts
Apelin levels inversely correlate with severity of heart failure in clinical studies
Methodology
Isolated rat heart perfusion studies, cardiomyocyte contractility assays, and APJ receptor signaling pathway analysis. Human heart failure tissue expression studies.
Limitations
Short half-life limits therapeutic application; analogs with improved stability under development. Human clinical trials in heart failure ongoing.
Protocols Using This Research
Tags
Educational use only. Research summaries are provided for informational purposes. Always consult the original publication and a qualified healthcare provider before making clinical decisions.
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