Potent and highly selective antagonist for the human adenosine A3
receptor, with low affinity for the rat A3
values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1
values are 4.1, 3.3 and 30 μ
M respectively) and > 1800-fold selectivity over rat A1
receptors. Acts as an inverse agonist in the [35
S binding assay in hA3
-CHO cells (IC50
= 4 nM). Produces thermal hyperalgesia in mice in vivo
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Medicinal chemistry of adenosine A3 receptor ligands.
2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and characterization of potent and selective inverse agonists at human A3 adenosine receptors.
Ozola et al.
Antinociceptive effects of novel A2B adenosine receptor antagonists.
Abo-Salem et al.