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Category:
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7TM Receptors Adenosine ReceptorsAntagonists
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Cat.No.
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Product Name
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2010 |
PSB 10 hydrochloride
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Price and Availability
Click here for full price details of
PSB 10
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Chemical Name:
8-Ethyl-1,4,7,8-tetrahydro-4-methyl-2-(2,3,5-trichlorop
henyl)-5H-imidazo[2,1-i]purin-5-one monohydrochloride |
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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.
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
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References:
Muller (2003) Medicinal chemistry of adenosine A3 receptor
ligands. Curr.Top.Med.Chem. 3 445. Ozola et al (2003)
2-Phenylimidazo[2,1-i]purin-5-ones: structure-activity relationships and
characterization of potent and selective inverse agonists at human A3
adenosine receptors. Bioorg.Med.Chem. 11 347. Abo-Salem et
al (2004) Antinociceptive effects of novel A2B adenosine
receptor antagonists. J.Pharmacol.Exp.Ther. 308 358.
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View related products by Pharmacological Action
or by Research Area
Keywords: PSB 10, Adenosine Receptors, Potent, Highly Selective Human A3 Receptor Antagonist / Inverse Agonist, PSB10, Tocris Bioscience
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