The field of therapeutic application of the A3 adenosine receptor (A3AR) antagonists represents a rapidly growing and intense area of research in the adenosine field. Even if there are currently no A3AR antagonists in clinical phases, in light of the plethora of biological effects attributed to A3ARs, substantial efforts in medicinal chemistry have been directed toward developing antagonists for the A3AR subtype. In this review, we summarize the more recent and promising evidences of the possible A3AR application as drug candidates, and the role of the receptor-driven design in their in silico characterization.
