Biological Activity
Partial agonist at the GABAA benzodiazepine site (EC50 = 10 nM at α1β1γ2 receptors). Displays anticonvulsive activity in vivo.
Compound Libraries
Bretazenil is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 418.28 |
| Formula | C19H20BrN3O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 84379-13-5 |
| PubChem ID | 107926 |
| InChI Key | LWUDDYHYYNNIQI-ZDUSSCGKSA-N |
| Smiles | O=C(N4[C@]([H])3CCC4)C1=C(Br)C=CC=C1N2C3=C(C(OC(C)(C)C)=O)N=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 | |||
| DMSO | 41.83 | 100 | |
| ethanol | 41.83 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 418.28. 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 | 2.39 mL | 11.95 mL | 23.91 mL |
| 5 mM | 0.48 mL | 2.39 mL | 4.78 mL |
| 10 mM | 0.24 mL | 1.2 mL | 2.39 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Rundfeldt et al (1995) Anticonvulsant tolerance and withdrawal characteristics of benzodiazepine receptor ligands in different seizure models in mice. Comparison of diazepam, bretazenil and abecarnil. J.Pharmacol.Exp.Ther. 275 693 PMID: 7473156
Munro et al (2008) Comparison of the novel subtype-selective GABAA receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models o J.Pharmacol.Exp.Ther. 327 969 PMID: 18791060
Puia et al (1992) Molecular mechanisms of the partial allosteric modulatory effects of bretazenil at γ-aminobutyric acid type A receptor. Proc.Natl.Acad.Sci. USA Neurobiology 89 3620 PMID:
Keywords: Bretazenil, supplier, benzodiazepines, partial, agonists, GABAA, receptors, Ro16-6028, Ro, 16-6028, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
