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Description: Potent and selective A1 antagonist
Chemical Name: 1-Butyl-8-(hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-3-(3-hydroxypropyl)-1H-purine-2,6-dione
Purity: ≥99% (HPLC)
Biological Activity
Potent and selective A1 adenosine receptor antagonist. Displays binding affinities of 0.12, 187, 552, 6500 and 2300 nM for rA1, hA2B, rA2A, rA3 and hA3 receptors respectively. Demonstrates greater selectivity than DPCPX (Cat. No. 0439).
Compound Libraries
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Technical Data
| M. Wt | 386.49 |
| Formula | C21H30N4O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 524944-72-7 |
| PubChem ID | 11689583 |
| InChI Key | CIBIXJYFYPFMTN-UHFFFAOYSA-N |
| Smiles | CCCCN1C(=O)N(CCCO)C2=C(NC(=N2)C23CC4CC2CC(C3)C4)C1=O |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.65 | 100 | |
| ethanol | 38.65 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 386.49. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.59 mL | 12.94 mL | 25.87 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.17 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Abo-Salem et al (2004) Antinociceptive effects of novel A2B adenosine receptor antagonists. J.Pharmacol.Exp.Ther 308 358 PMID: 14563788
Weyler et al (2006) Improving potency, selectivity, and water solubility of adenosine A1 receptor antagonists: xanthines modified at position 3 and related pyrimido[1,2,3-cd]purinediones. Chem.Med.Chem. 1 891
If you know of a relevant reference for PSB 36, please let us know.
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Keywords: PSB 36, PSB 36 supplier, Potent, selective, A1, antagonists, Receptors, adenosines, PSB36, Adenosine, 2019, Tocris Bioscience
5 Citations for PSB 36
Citations are publications that use Tocris products. Selected citations for PSB 36 include:
Carlström et al (2010) Adenosine A(2) receptors modulate tubuloglomerular feedback. Am J Physiol Renal Physiol 299 F412 PMID: 20519378
Arnal et al (2013) Influence of age, body temperature, GABAA receptor inhibition and caffeine on the Hering-Breuer inflation reflex in unanesthetized rat pups. Respir Physiol Neurobiol 186 73 PMID: 23318703
Cheng et al (2017) Structures of Human A1 and A2A Adenosine Receptors with Xanthines Reveal Determinants of Selectivity. Structure 25 1275 PMID: 28712806
Guerreiro et al (2008) Paraxanthine, the primary metabolite of caffeine, provides protection against DArgic cell death via stimulation of ryanodine receptor channels. Mol Pharmacol 74 980 PMID: 18621927
Ziemlinska et al (2014) Overexpression of BDNF increases excitability of the lumbar spinal network and leads to robust early locomotor recovery in completely spinalized rats. PLoS One 9 e88833 PMID: 24551172
Do you know of a great paper that uses PSB 36 from Tocris? Please let us know.
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