Adenosine kinase is the key metabolizing enzyme regulating cellular adenosine concentrations. Inhibition of adenosine kinase can selectively enhance the protective actions of adenosine during tissue trauma without producing the nonspecific effects associated with the systemic administration of adenosine receptor agonists (IC50: 1.7 nM in cell-free assays).

Adenosine Kinase Inhibitor was found to be a potent non-nucleoside adenosine kinase inhibitor with several folds of magnitude selectivity over other sites of adenosine interaction. Adenosine Kinase Inhibitor was 1300- to 7700-fold selective for adenosine kinase compared with other neurotransmitters and peptide receptors, neurotransmitter/nucleoside reuptake sites, and enzymes. Adenosine Kinase Inhibitor was equipped in inhibiting native human adenosine kinase, human recombinant isoforms, as well as adenosine kinase from dog, rat, monkey, and mouse brain [1].

Adenosine Kinase Inhibitor was orally active and efficacious in reducing acute somatic nociception in the mouse hot-plate assay. Adenosine Kinase Inhibitor could dose-dependently reduce nociception in the phenyl-p-quinone-induced abdominal constriction assay. The antinociceptive effects of Adenosine Kinase Inhibitor in the hotplate assay were stopped by the nonselective adenosine receptor antagonist theophylline, but not by a peripherally selective adenosine receptor antagonist [1].