Adenosine A2A Receptor as a Drug Discovery Target

摘要

The adenosine A_(2A) receptor is a G-protein-coupled receptor (GPCR) that has been extensively studied during the past few decades because it offers numerous possibilities for therapeutic applications. Herein we describe adenosine A_(2A) receptor distribution, signaling pathways, pharmacology, and molecular structure, followed by a summary and SAR discussion of the most relevant series of adenosine A_(2A) agonists and antagonists. This review also provides an update of the A_(2A) ligands that are undergoing or have undergone clinical studies, including the two currently marketed agonists adenosine and regadenoson.