Potent and selective antagonist for the human adenosine A3
receptor, with low affinity for the rat A3
values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A1
values are 4.1 and 3.3 μ
M respectively) and > 180-fold selectivity over rat A1
, rat A2A
and mouse A2B
receptors. Acts as an inverse agonist in the [35
S binding assay in hA3
-CHO cells (IC50
= 36 nM).
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.
Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A- and A3-adenosine receptor antagonists.
Muller et al.
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.