ABT-702 is a potent, selective, orally active, non-nucleoside adenosine kinase (ADK) inhibitor with IC50 of 1.7 nM.
ABT-702 displays several orders of magnitude selectivity over other sites of ADO interaction (A(1), A(2A), A(3) receptors, ADO transporter, and ADO deaminase), and 1300- to 7700-fold selective for ADK compared with a number of other neurotransmitter and peptide receptors, ion channel proteins, neurotransmitter/nucleoside reuptake sites, and enzymes, including COX-1 and -2.
ABT-702 is orally active and fully efficacious in reducing acute somatic nociception (ED50 = 8 micromol/kg i.p.; 65 micromol/kg p.o.) in the mouse hot-plate assay.
ABT-702 also dose dependently reduced nociception in the phenyl-p-quinone-induced abdominal constriction assay.
ABT-702 dispalyed analgesic and anti-inflammatory properties in vivo.
