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Submit ReviewBretazenil
Description: Benzodiazepine partial agonist
Alternative Names: Ro 16-6028
Chemical Name: (13aS)-8-Bromo-11,12,13,13a-tetrahydro-9-oxo-9H-imidazo[1,5-a]pyrrolo[2,1-c][1,4]benzodiazepine-1-carboxylic acid 1,1-dimethylethyl ester
Purity: ≥98% (HPLC)
Biological Activity for Bretazenil
Bretazenil is a partial agonist at the GABAA benzodiazepine site (EC50 = 10 nM at α1β1γ2 receptors). Displays anticonvulsive activity in vivo.
Technical Data for Bretazenil
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Bretazenil
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.83 | 100 | |
| ethanol | 41.83 | 100 |
Preparing Stock Solutions for Bretazenil
The following data is based on the product molecular weight 418.28. 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 | 2.39 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 for Bretazenil
References for Bretazenil
References are publications that support the biological activity of the product.
Rundfeldt et al (1995) Anticonvulsant tolerance and withdrawal characteristics of benzodiazepine receptor ligands in different seizure models in mice. Comparison of D.pam, 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 D.pam, zolpidem, bretazenil, and gaboxadol in rat models of i 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
If you know of a relevant reference for Bretazenil, please let us know.
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Keywords: Bretazenil, Bretazenil supplier, benzodiazepines, partial, agonists, GABAA, receptors, Ro16-6028, Ro, 16-6028, Receptors, 3568, Tocris Bioscience
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Literature in this Area
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