Adenosine receptors belong to a class of integral membrane proteins known as G-protein-coupled receptors (GPCRs). Members of this class of proteins have seven membrane-spanning α-helices with an extracellular amino terminus and an intracellular carboxy-terminal tail. Adenosine receptors are receptors for adenosine, which is an endogenous nucleoside modulator that exists ubiquitously and modulates many body functions. The four known subtypes are denoted as A1, A2A, A2B, and A3.
These receptors differ in their affinity for adenosine, in the type of G proteins that they recruit, and in the downstream signaling pathways that are activated in the target cells. These receptors are important mediators of cellular signaling, which play vital roles in protecting tissue and organs from damage. Many pathophysiological conditions are believed to be associated with adenosine and their receptors such as asthma, neurodegenerative disorders, chronic inflammatory diseases, and cancer. As a result, adenosine receptor-selective ligands, including agonists and antagonists, have been developed for the treatment of pain, ischemic conditions, glaucoma, asthma, arthritis, cancer, and other disorders in which inflammation is a feature.
Here we give an introduction of different adenosine receptor subtypes in terms of their properties, functions, and applications. Each of them shows a distinct tissue distribution and has been found to be responsible for specific actions and physiological processes. They have been actively studied for different purposes.
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