PSB 10 hydrochloride

Biological Activity

PSB 10 hydrochloride is a potent and highly selective antagonist for the human adenosine A₃ receptor, with low affinity for the rat A₃ receptor (K_i values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A₁, A_2A and A_2B receptors (K_i values are 4.1, 3.3 and 30 μM respectively) and > 1800-fold selectivity over rat A₁ and A_2A 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

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. Human 3D vascularized organotypic microfluidic assays to study breast cancer cell extravasation.
   Jeon, Jessie S, Bersini, Simone, Gilardi, Mara, Dubini, Gabriele, Charest, Joseph L, Moretti, Matteo, Kamm, Roger D
   Proc Natl Acad Sci U S A, 2015;112(1):214-9.
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
4. Antinociceptive effects of novel A_2B adenosine receptor antagonists.
   Abo-Salem et al.
   J.Pharmacol.Exp.Ther., 2004;308:358

Product Datasheets