A noncompetitive antagonist and inverse agonist of mGluR5
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Fenobam (hydrate)

Item No. 29759

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(3-chlorophenyl)-N′-(4,5-dihydro-1-methyl-4-oxo-1H-imidazol-2-yl)-urea, monohydrate
CAS Number
63540-28-3
Molecular Formula
C11H11ClN4O2 • H2O
Formula Weight
284.7
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mM
λmax
214, 271 nm
SMILES
ClC1=CC=CC(NC(NC(N(C)C2)=NC2=O)=O)=C1.O
InChi Code
InChI=1S/C11H11ClN4O2.H2O/c1-16-6-9(17)14-10(16)15-11(18)13-8-4-2-3-7(12)5-8;/h2-5H,6H2,1H3,(H2,13,14,15,17,18);1H2
InChi Key
UNFQKKSADLVQJE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $169

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    Product Description

    Fenobam is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5) that binds to an allosteric site.1 It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate (Item No. 20211) in HEK293 cells expressing the human receptor (IC50 = 58 nM) and inhibits basal activity of mGluR5 in a cell-based assay (IC50 = 84 nM).1 Fenobam (10 and 30 mg/kg) reduces stress-induced hyperthermia in mice and increases drinking time in the Vogel conflict test in rats when administered at a dose of 30 mg/kg, indicating anxiolytic-like activity. It induces analgesia in the formalin test in mice when administered at a dose of 30 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Porter, R.H.P., Jaeschke, G., Spooren, W., et al. Fenobam: A clinically validated nonbenzodiazepine anxiolytic Is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J. Pharmacol. Exp. Ther. 315(2), 711-721 (2005).

    2. Montana, M.C., Conrardy, B.A., Cavallone, L.F., et al. Metabotropic glutamate receptor 5 antagonism with fenobam: Examination of analgesic tolerance and side effect profile in mice. Anesthesiology 115(6), 1239-1250 (2011).