Abstract
Adenosine is an endogenous nucleoside which strongly impacts the cardiovascular system. Adenosine is released mostly by endothelial cells and myocytes during ischemia or hypoxia and greatly regulates the cardiovascular system via four specific G-protein-coupled receptors named A1R, A2AR, A2BR, and A3R. Among them, A2 subtypes are strongly expressed in coronary tissues, and their activation increases coronary blood flow via the production of cAMP in smooth muscle cells. A2A receptor modulators are an opportunity for intense research by the pharmaceutical industry to develop new cardiovascular therapies. Most innovative therapies are mediated by the modulation of adenosine release and/or the activation of the A2A receptor subtypes. This review aims to focus on the specific exploration of the adenosine plasma level and its relationship with the A2A receptor, which seems a promising biomarker for a diagnostic and/or a therapeutic tool for the screening and management of coronary artery disease. Finally, a recent class of selective adenosine receptor ligands has emerged, and A2A receptor agonists/antagonists are useful tools to improve the management of patients suffering from coronary artery disease.
Highlights
Adenosine, a nucleoside that is an ATP derivative, is found in most vascular beds of mammalian species
A2AR is strongly expressed in myocytes in humans, and its activation leads to the myorelaxation of smooth muscle cells and vasodilation, increasing the coronary blood flow [18] partly via cAMP production in smooth muscle cells, cAMP production and coronary vasodilation being correlated [19]
Open-label, randomized study named “The Acute Myocardial Infarction STudy ADenosine The Acute Myocardial Infarction STudy Adenosine” (AMISTAD) of patients treated with thrombolysis for ST-elevation myocardial infarction (STEMI), the intravenous administration of adenosine failed to reduce the infarct size and improve clinical outcomes [56]
Summary
A nucleoside that is an ATP derivative, is found in most vascular beds of mammalian species. The effects of adenosine on coronary blood flow are thought to be mediated primarily by the activation of A2 receptors [3,4,5], and mostly via the A2A R subtype [6]. This vasorelaxation decreases vascular resistance, thereby facilitating coronary blood flow and oxygen delivery. This article reviews the most recent advances in emerging data on circulating plasma adenosine and its relationship with the A2A receptor in coronary artery and ischemic heart diseases
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