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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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2012 |
PSB 11 hydrochloride
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Price and Availability
Click here for full price details of
PSB 11
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Chemical Name:
(8R)-8-Ethyl-1,4,7,8-tetrahydro-4-5H-imidazo[2,1-i]puri
n-5-one hydrochloride |
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Biological Activity:
Potent and selective antagonist for
the human adenosine A3 receptor, with low affinity for the rat A3
receptor (Ki values are 2.3 and > 10000 nM respectively).
Displays > 1000-fold selectivity over human A1 and A2A
receptors (Ki values are 4.1 and 3.3 μM
respectively) and > 180-fold selectivity over rat A1, rat A2A
and mouse A2B receptors. Acts as an inverse agonist in the [35S]GTPγS
binding assay in hA3-CHO cells (IC50 = 36 nM).
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Technical Data:
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Resources:
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Certificate of Analysis / MSDS:
Certificate of Analysis is currently unavailable on-line. Please contact Customer Service
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References:
Muller et al (2002) Imidazo[2,1-i]purin-5-ones and related tricyclic
water-soluble purine derivatives: potent A2A- and A3-adenosine
receptor antagonists. J.Med.Chem. 45 3440. 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.
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View related products by Pharmacological Action
or by Research Area
Keywords: PSB 11, Adenosine Receptors, Potent, Selective Human A3 Receptor Antagonist / Inverse Agonist, PSB11, Tocris Bioscience
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