PSB 10 hydrochloride

• Supplier: Tocris Bioscience
• Catalog: 3199
• Prices: $189.00, $765.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 591771-91-4
• Chemical Name: 8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorophenyl)-5H-imidazo[2,1-i]purin-5-onemonohydrochloride
• Formula: C16H14Cl3N5O.HCl
• Molecular Weight: 435.14
• Purity: >98 %
• Description: Potent and highly selective antagonist for the human adenosine A 3 receptor, with low affinity for the rat A 3 receptor (K i values are 0.44 and > 17000 nM respectively). Displays > 3800-fold selectivity over human A 1 , A 2A and A 2B receptors (K i values are 4.1, 3.3 and 30 μ M respectively) and > 1800-fold selectivity over rat A 1 and A 2A receptors. Acts as an inverse agonist in the [ 35 S]GTP γ S binding assay in hA 3 -CHO cells (IC 50 = 4 nM). Produces thermal hyperalgesia in mice in vivo .

Product References

Medicinal chemistry of adenosine A3 receptor ligands. - Medicinal chemistry of adenosine A3 receptor ligands.

Muller CE. Curr Top Med Chem. 2003;3(4):445-62.

2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and - 2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and

Ozola V, Thorand M, Diekmann M, Qurishi R, Schumacher B, Jacobson KA, Muller CE. Bioorg Med Chem. 2003 Feb 6;11(3):347-56.

Antinociceptive effects of novel A2B adenosine receptor antagonists. - Antinociceptive effects of novel A2B adenosine receptor antagonists.

Abo-Salem OM, Hayallah AM, Bilkei-Gorzo A, Filipek B, Zimmer A, Muller CE. J Pharmacol Exp Ther. 2004 Jan;308(1):358-66. Epub 2003 Oct 16.