Biological Activity
Selective α2A-adrenoceptor antagonist (Ki = 1.7 nM and 144.5 nM at α2A and α2B-adrenergic receptors respectively). Increases hippocampal noradrenalin release following systemic administration. Also available as part of the α2-Adrenoceptor Tocriset™.
Licensing Information
Sold with the permission of GlaxoSmithKline
Technical Data
| M. Wt | 331.37 |
| Formula | C13H17N3.C4H4O4 |
| Storage | Desiccate at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 681806-46-2 |
| PubChem ID | 10382026 |
| InChI Key | DDIQGSUEJOOQQQ-BTJKTKAUSA-N |
| Smiles | OC(=O)C=C/C(O)=O.CC1N(CC2=NCCN2)CC2=C1C=CC=C2 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| phosphate buffered saline | 33.14 | 100 | |
| water | 33.14 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 331.37. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 3.02 mL | 15.09 mL | 30.18 mL |
| 5 mM | 0.6 mL | 3.02 mL | 6.04 mL |
| 10 mM | 0.3 mL | 1.51 mL | 3.02 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.6 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Callado et al (1999) α2A-But not α2B/C-adrenoceptors modulate noradrenaline release in rat locus coeruleus: voltammetric data. Eur.J.Pharmacol. 366 35 PMID: 10064149
Gavin et al (1997) α2C-adrenoceptors mediate contractile responses to noradrenaline in the human saphenous vein. Naunyn Schmiedebergs Arch.Pharmacol. 355 406 PMID: 9089673
Kiss et al (1995) Subtype-specificity of the presynaptic α2-adrenoceptors modulating hippocampal norepinephrine release in rat. Brain Res. 674 238 PMID: 7796102
Young et al (1989) Novel α2-adrenoceptor antagonists show selectivity for α2A- and α2B-adrenoceptor subtypes. Eur.J.Pharmacol. 168 381 PMID: 2573535
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