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)
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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.
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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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Porteret 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
Montanaet 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
Porteret al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 267 PMID:
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