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

Uses

PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice[1][2].

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 .

in vivo

storage

Desiccate at +4°C

References

[1] Ozola V, et, al. 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at Human A3 adenosine receptors. Bioorg Med Chem. 2003 Feb 6;11(3):347-56. DOI:10.1016/s0968-0896(02)00456-x
[2] Abo-Salem OM, et, al. Antinociceptive effects of novel A2B adenosine receptor antagonists. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66. DOI:10.1124/jpet.103.056036