Therapeutic potential of A2 adenosine receptor pharmacological regulators in the treatment of cardiovascular diseases, recent progress, and prospective

Abstract

Adenosine and its analogs are of particular interest as potential therapeutic agents for treatment of cardiovascular diseases (CVDs). A2 adenosine receptor subtypes (A2a and A2b) are extensively expressed in cardiovascular system, and modulation of these receptors using A2 adenosine receptor agonists or antagonists regulates heart rate, blood pressure, heart rate variability, and cardiovascular toxicity during both normoxia and hypoxia conditions. Regulation of A2 adenosine receptor signaling via specific and novel pharmacological regulators is a potentially novel therapeutic approach for a better understanding and hence a better management of CVDs. This review summarizes the role of pharmacological A2 adenosine receptor regulators in the pathogenesis of CVDs.

Adenosine Receptor Profiling Reveals an Association between the Presence of Spare Receptors and Cardiovascular Disorders

“…The adenosinergic system also plays a key role in cardiovascular pathophysiology, as adenosine receptors are expressed on most cell types in the cardiovascular system such as cardiomyocytes, endothelial cells, vascular smooth muscle cells, pericytes, and fibroblasts [1]. Adenosine receptors have been therefore evaluated as targets for the development of new therapeutic or diagnosis options for the cardiovascular system [2,3,4,5]. The goal of this review is to present experimental evidence supporting the existence and implication in cardiovascular disorders of specific adenosinergic pharmacological profiles agreeing with the concept of “receptor reserve” also known as “spare receptors” [6].…”

Modulation of Blood–Brain Barrier Permeability by Activating Adenosine A2 Receptors in Oncological Treatment

“…The effectiveness of this method in modulating BBB has already been proven for the agonists of the bradykinin B2 receptor—RMP-7 [ 111 ]. In turn, the intrathecal injection of an adenosine agonist (A2 agonist-CPCA) influenced the cardiovascular system, causing a decrease of blood pressure and heart rate in rats [ 112 ]. A promising direction seems to be the synthesis of nanoparticles functionalized with ligands, e.g., antibodies.…”

<p>Nanoparticle-Mediated Drug Delivery for the Treatment of Cardiovascular Diseases</p>

“…It has studied that the dysfunction of these receptors stimulates CVDs, but the exact pathological mechanisms behind these A2 receptors are not available so far. 46 Stem cell transplantation has received much attention for balancing and regulating cardiac properties. Several studies indicated that stem cells could improve the heart functions through their release of paracrine signals and then networking with tissues or organs.…”