Fenobam

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Cat.No. 2386 - Fenobam | C11H11N4O2Cl | CAS No. 57653-26-6
Description: Potent and selective mGlu5 antagonist
Chemical Name: N-(3-Chlorophenyl)-N'-(4,5-dihydro-1-methyl-4-oxo-1H-imidazol-2-yl)urea
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature

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

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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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

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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References

References are publications that support the biological activity of the product.

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


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Keywords: Fenobam, Fenobam supplier, Potent, selective, mGlu5, antagonist, mGluR5, antagonists, Group, I, Receptors, Glutamate, Metabotropic, (Metabotropic), 2386, Tocris Bioscience

1 Citation for Fenobam

Citations are publications that use Tocris products. Selected citations for Fenobam include:

Crock et al (2012) Metabotropic glutamate receptor 5 (mGluR5) regulates bladder nociception. Mol Pain 8 20 PMID: 22449017


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


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