FenobamA potent and selective non-competitive mGluR5 antagonist

Fenobam (CAS 57653-26-6)

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Application: A potent and selective non-competitive mGluR5 antagonist
CAS Number: 57653-26-6
Purity: ≥98%
Molecular Weight: 266.69
Molecular Formula: C11H11ClN4O2
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* Refer to Certificate of Analysis for lot specific data (including water content).
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Fenobam is a selective non-competitive antagonist of the mGluR-5 receptor (metabotropic glutamate receptor subtype 5). This compound is described to act at an allosteric modulatory site on mGluR-5 common with MPEP (sc-215392), producing inverse agonist activity. Interaction of Fenobam at mGluR-5 is correlated to anxiolytic effects.


References

1. Goldberg, M.E., et al. 1983. Neuropharmacology. 22: 1499-1504. PMID: 6142427
2. Wu, W.N., et al. 1995. J Pharm Sci. 84: 185-189. PMID: 7738798
3. Porter, R.H., et al. 2005. J. Pharmacol. Exp. Ther. 315: 711-721. PMID: 16040814
4. Wållberg, A., et al. 2006. Bioorg. Med. Chem. Lett. 16: 1142-1145. PMID: 16380255

Physical State :
Solid
Solubility :
Soluble in methanol, and DMSO (100 mM).
Storage :
Store at 4° C
Density :
1.48 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
mGlu5 constitutive activity: IC50 = 87 nM
Ki Data :
Metabotropic glutamate receptor 1: Ki= 6.7 nM (human)
pK Values :
pKa: 8.32 (Predicted), pKb: 1.84 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
YS6205000
PubChem CID :
162834
MDL Number :
MFCD00868019
SMILES :
CN1CC(=O)N=C1NC(=O)NC2=CC(=CC=C2)Cl

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Certificate of Analysis

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