Cat. No. 2009
Chemical Name: 4-(2,3,6,7-Tetrahydro-2,6-dioxo-1-p
Biological ActivityHighly selective, water-soluble, human A2B adenosine receptor antagonist. Ki values are 53.4, > 10000 and > 10000 nM at human A2B, A1 and A3 receptors respectively. Also selective versus rat A1 and A2A receptors (Ki values are 2200 and 24000 nM respectively). Produces potent analgesic effects in vivo.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther. 308 358. PMID: 14563788.
Yan and Muller (2004) Preparation, properties, reactions, and adenosine receptor affinities of sulfophenylxanthine nitrophenyl esters: toward the development of sulfonic acid prodrugs with peroral bioavailability. J.Med.Chem. 47 1031. PMID: 14761205.
Hayallah et al (2002) 1,8-Disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists. J.Med.Chem. 45 1500. PMID: 11906291.
Muller et al (1998) 8-(Sulfostyryl)xanthines: water-soluble A2A-selective adenosine receptor antagonists. Bioorg.Med.Chem. 6 707. PMID: 9681137.
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Citations are publications that use Tocris products. Selected citations for PSB 1115 include:
Ning et al (2014) Excess adenosine A2B receptor signaling contributes to priapism through HIF-1α mediated reduction of PDE5 gene expression. FASEB J 28 2725. PMID: 24614760.
Rao et al (2014) A dual role for autophagy in a murine model of lung cancer. Proc Natl Acad Sci U S A 5 3056. PMID: 24445999.
Chia et al (2013) The protective effects of CD39 overexpression in multiple low-dose streptozotocin-induced diabetes in mice. J Clin Invest 62 2026. PMID: 23364452.
Iannone et al (2013) Blockade of A2b adenosine receptor reduces tumor growth and immune suppression mediated by myeloid-derived suppressor cells in a mouse model of melanoma. Neoplasia 15 1400. PMID: 24403862.
Hua et al (2011) IL-4 amplifies the pro-inflammatory effect of adenosine in human mast cells by changing expression levels of adenosine receptors. PLoS One 6 e24947. PMID: 21966389.
Stagg et al (2010) Anti-CD73 antibody therapy inhibits breast tumor growth and metastasis. J Immunol 107 1547. PMID: 20080644.
Frick et al (2009) Contribution of adenosine A2B receptors to inflammatory parameters of experimental colitis. J Pharmacol Exp Ther 182 4957. PMID: 19342675.
Hart et al (2009) Cutting Edge: A2B Adenosine receptor signaling provides potent protection during intestinal ischemia/reperfusion injury. Diabetes 182 3965. PMID: 19299692.
Eckle et al (2008) A2B adenosine receptor signaling attenuates acute lung injury by enhancing alveolar fluid clearance in mice. J Immunol 118 3301. PMID: 18787641.
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Keywords: PSB 1115, supplier, Selective, human, A2B, receptors, antagonists, water-soluble, adenosines, PSB1115, Tocris Bioscience, Adenosine A2B Receptor Antagonist products