A2A Adenosine Receptor and its Modulators: Overview on a Druggable GPCR and on Structure-Activity Relationship Analysis and Binding Requirements of Agonists and Antagonists

• Published in: Current pharmaceutical design Vol. 14; no. 15; pp. 1525 - 1552
• Main Authors: Cristalli, G., Lambertucci, C., Marucci, G., Volpini, R., Ben, D.
• Format: Journal Article
• Language: English
• Published: United Arab Emirates Bentham Science Publishers Ltd 01.05.2008
• Subjects: Adenine - analogs & derivatives; Adenine - chemistry; Adenine - pharmacology; Adenosine - analogs & derivatives; Adenosine - chemistry; Adenosine - pharmacology; Adenosine A2 Receptor Agonists; Adenosine A2 Receptor Antagonists; Animals; Drug Design; Drug Partial Agonism; Humans; Ligands; Neuroprotective Agents - chemistry; Neuroprotective Agents - pharmacology; Protein Conformation; Radiopharmaceuticals - chemistry; Radiopharmaceuticals - metabolism; Receptor, Adenosine A2A - chemistry; Structure-Activity Relationship; Xanthines - chemistry; Xanthines - pharmacology

Since the discovery of the biological effects of adenosine, the development of potent and selective agonists and antagonists of adenosine receptors has been the subject of medicinal chemistry research for several decades, even if their clinical evaluation has been discontinued. Main problems include...