Chapter 5 - Biochemical Characterization of Adenosine Agonists and Antagonists

Abstract

This chapter discusses the binding characterization of adenosine receptor ligands and the signal transduction for each subtype. Usually, the emphasis is laid on adenosine A2A receptor antagonists and the biochemical basis of their application to the therapy of Parkinson's disease. The identification of adenosine receptor subtypes has been made according to the order of affinity along with the functional activity of the receptor ligands. This method can be useful in combination with molecular biology because most cells and tissues express at least two subtypes of adenosine receptors. The development of selective agonists and antagonists for the A1 and A2A adenosine receptor subtypes has opened up the possibility that these receptors could be promising molecular targets for therapeutics in disorders like cardiovascular disease, inflammatory disease and so on. Last but not the least, pharmacological investigations using ligands have led to the recognition of adenosine receptors as one of the most promising and pioneering molecular targets for therapeutics.