8-ETHYL-1,4,7,8-TETRAHYDRO-4-METHYL-2-(2,3,5-TRICHLOROPHENYL)-5H-IMIDAZO[2,1-I]PURIN-5-ONE MONOHYDROCHLORIDE

Biological Activity

Potent and highly selective antagonist for the human adenosine A 3 receptor, with low affinity for the rat A 3 receptor (K i values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A 1 , A 2A and A 2B receptors (K i values are 4.1, 3.3 and 30 μ M respectively) and > 1800-fold selectivity over rat A 1 and A 2A receptors. Acts as an inverse agonist in the [ 35 S]GTP γ S binding assay in hA 3 -CHO cells (IC 50 = 4 nM). Produces thermal hyperalgesia in mice in vivo .

storage

Desiccate at +4°C