Biological Activity
Potent and selective non-competitive mGlu5 antagonist that displays inverse agonist properties; blocks mGlu5 constitutive activity in vitro (IC50 = 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties.
Compound Libraries
Fenobam is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 266.69 |
| Formula | C11H11N4O2Cl |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 57653-26-6 |
| PubChem ID | 162834 |
| InChI Key | DWPQODZAOSWNHB-UHFFFAOYSA-N |
| Smiles | CN1CC(=O)N=C1NC(=O)NC1=CC(Cl)=CC=C1 |
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 | 26.67 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 266.69. 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 | 3.75 mL | 18.75 mL | 37.5 mL |
| 5 mM | 0.75 mL | 3.75 mL | 7.5 mL |
| 10 mM | 0.37 mL | 1.87 mL | 3.75 mL |
| 50 mM | 0.07 mL | 0.37 mL | 0.75 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Porter et al (2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 315 711 PMID: 16040814
Montana et al (2009) The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine. J.Pharmacol.Exp.Ther. 330 834 PMID: 19515968
Porter et al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 267 PMID:
Keywords: Fenobam, supplier, Potent, selective, mGlu5, antagonist, mGluR5, antagonists, Group, I, Receptors, Glutamate, Metabotropic, Glutamate, (Metabotropic), Group, I, Receptors, Glutamate, (Metabotropic), Group, I, Receptors, Tocris Bioscience
