PSB 11 hydrochloride

Biological Activity

PSB 11 hydrochloride is a potent and selective antagonist for the human adenosine A₃ receptor, with low affinity for the rat A₃ receptor (K_i values are 2.3 and > 10000 nM respectively). Displays > 1000-fold selectivity over human A₁ and A_2A receptors (K_i values are 4.1 and 3.3 μM respectively) and > 180-fold selectivity over rat A₁, rat A_2A and mouse A_2B receptors. Acts as an inverse agonist in the [³⁵S]GTPγS binding assay in hA₃-CHO cells (IC₅₀ = 36 nM).

Technical Data

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

1. Imidazo[2,1-i]purin-5-ones and related tricyclic water-soluble purine derivatives: potent A_2A- and A₃-adenosine receptor antagonists.
   Muller et al.
   J.Med.Chem., 2002;45:3440
2. Medicinal chemistry of adenosine A₃ receptor ligands.
   Muller
   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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