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Description: Potent and selective mGlu5 negative allosteric modulator (NAM)
Chemical Name: N-(3-Chlorophenyl)-N'-(4,5-dihydro-1-methyl-4-oxo-1H-imidazol-2-yl)urea
Purity: ≥99% (HPLC)
Citations (1)
Literature (5)

Biological Activity for Fenobam

Fenobam is a potent and selective non-competitive mGlu5 negative allosteric modulator (NAM) that also 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 for Fenobam

Fenobam is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for Fenobam

M. Wt 266.69
Formula C11H11N4O2Cl
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 57653-26-6
PubChem ID 162834
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 for Fenobam

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 26.67 100

Preparing Stock Solutions for Fenobam

The following data is based on the product molecular weight 266.69. 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 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 for Fenobam

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

Kufahl et al (2013) Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine F1000Res. 1 10.12688/f1000resear PMID: 24358885

Liu et al (2018) Orthosteric and allosteric action of the C5a receptor antagonists Nature Structural & Molecular Biology 25 472 PMID: 29867214

If you know of a relevant reference for Fenobam, please let us know.

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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

Do you know of a great paper that uses Fenobam from Tocris? Please let us know.

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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.

Metabotropic Glutamate Receptors Scientific Review

Metabotropic Glutamate Receptors Scientific Review

Written by Francine Acher, this review discusses the pharmacology and therapeutic potential of mGlu receptors, and the compounds acting upon them; compounds available from Tocris are listed.

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