Development of potent and selective human A3 adenosine receptor agonists.

Abstract

On the basis of bioisosteric rationale, structure-activity relationship of Cl-IB-MECA, which showed high binding affinity at the human A3 adenosine receptor, was studied. From this study, 2-chloro-4'-thioadenosine-5'-methyluronamide was discovered as the most potent and selective agonist at the human A3 adenosine receptor.