Biological Activity
High affinity benzodiazepine ligand. Ki values are 3.1 and 5.3 nM for diazepam-insensitive (DI) and diazepam-sensitive (DS) benzodiazepine receptors respectively. Acts as partial inverse agonist at recombinant DS α1-, α2-, α3- and α5-GABAA receptors. Displays partial agonism at DI α4- and α6-GABAA receptors. Antagonizes several behavioral and neurochemical effects of ethanol. Proconvulsant and anxiogenic.
Technical Data
| M. Wt | 326.31 |
| Formula | C15H14N6O3 |
| Storage | Desiccate at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 91917-65-6 |
| PubChem ID | 5081 |
| InChI Key | CFSOJZTUTOQNIA-UHFFFAOYSA-N |
| Smiles | CCOC(=O)C1=C2CN(C)C(=O)C3=C(C=CC(=C3)N=[N+]=[N-])N2C=N1 |
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 | 3.26 | 10 | |
| ethanol | 1.63 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 326.31. 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 | 3.06 mL | 15.32 mL | 30.65 mL |
| 5 mM | 0.61 mL | 3.06 mL | 6.13 mL |
| 10 mM | 0.31 mL | 1.53 mL | 3.06 mL |
| 50 mM | 0.06 mL | 0.31 mL | 0.61 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Suzdak et al (1986) A selective imidazobenzodiazepine antagonist of ethanol in the rat. Science 234 1243 PMID: 3022383
Wong and Skolnick (1992) High affinity ligands for 'diazepam-insensitive' benzodiazepine receptors. Eur.J.Pharmacol. 225 63 PMID: 1311690
Knoflach et al (1996) Pharmacological modulation of the diazepam-insensitive recombinant gamma-aminobutyric acidA receptors alpha 4 beta 2 gamma 2 and alpha 6 beta 2 gamma 2. Mol.Pharmacol. 50 1253 PMID: 8913357
Keywords: Ro 15-4513, supplier, Benzodiazepine, partial, inverse, agonists, GABAA, Receptors, Ro15-4513, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
