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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)
Literature (2)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

Citations for Bretazenil

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.