Chemical and pharmacological profile of selective adenosine receptor agonists

Abstract

This chapter discusses the chemical and pharmacological profile of selective adenosine receptor agonists. There is evidence that the purine nucleoside adenosine specifically modulates neurotransmission through the interaction with four cell surface receptors recently classified as A1, A2a, A2b, and A3. These receptor subtypes have been cloned and characterized as belonging to the super family of receptors with seven transmembrane helices that couple to G proteins. The chapter reports contributions to the improvement of structure-activity relationships as well as to the development of A1 and A2a potent and selective agonists. The chapter investigates the role of the purine nitrogens on adenosine activity. Several deaza analogues of adenosine were therefore synthesized and tested for affinity at A1 and A2a receptors in radioligand binding studies and for their activity as inhibitors of human platelet aggregation.