Catalog Number: 2012
Chemical Name: (8R)-8-Ethyl-1,4,7,8-tetrahydro-4-5H-imidazo[2,1-i]purin-5-one hydrochloride
Biological Activity
Potent and selective antagonist for the human adenosine A3 receptor, with low affinity for the rat A3 receptor (Ki values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A1 and A2A receptors (Ki values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A1, rat A2A and mouse A2B receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 36 nM).
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 20 mM in DMSO with gentle warming
  • Purity:
  • Storage:
    Store at +4°C
  • CAS No:
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.
Background References
  1. Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A2A- and A3-adenosine receptor antagonists.
    Muller et al.
    J.Med.Chem., 2002;45:3440
  2. Medicinal chemistry of adenosine A3 receptor ligands.
    Curr.Top.Med.Chem., 2003;3:445
  3. 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.
    Bioorg.Med.Chem., 2003;11:347
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