Catalog Number: 2010
Chemical Name: 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 A3 receptor, with low affinity for the rat A3 receptor (Ki values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A1, A2A and A2B receptors (Ki values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A1 and A2A receptors. Acts as an inverse agonist in the [35S]GTPγS binding assay in hA3-CHO cells (IC50 = 4 nM). Produces thermal hyperalgesia in mice in vivo.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 25 mM in DMSO and to 10 mM in ethanol
  • Purity:
  • Storage:
    Desiccate 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. Medicinal chemistry of adenosine A3 receptor ligands.
    Curr.Top.Med.Chem., 2003;3:445
  2. 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
  3. Antinociceptive effects of novel A2B adenosine receptor antagonists.
    Abo-Salem et al.
    J.Pharmacol.Exp.Ther., 2004;308:358
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