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Fenobam

mGluR5 antagonist
 
ALX-550-413-M005 5 mg 69.00 USD
 
ALX-550-413-M025 25 mg 289.00 USD
Do you need bulk/larger quantities?
 
Potent and selective non-competitive mGluR5 antagonist that displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC50=87nM). Acts at an allosteric modulatory site shared with MPEP (Prod. No. ALX-550-368) and binds mGluR5 with Kd values of 54nM and 31nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo.

Product Specification

Formula:C11H11ClN4O2
 
MW:266.7
 
CAS:57653-26-6
 
Purity:≥98% (1H-NMR)
 
Identity:Determined by NMR.
 
Appearance:Off-white to pale orange solid.
 
Solubility:Soluble in DMSO or methanol.
 
Shipping:Ambient
 
Long Term Storage:+4°C
 
550-413
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550-413

Product Literature References

Phenyl ureas of creatinine as mGluR5 antagonists. A structure-activity relationship study of fenobam analogues: A. Wallberg et al.; Bioorg. Med. Chem. Lett. 16, 1142 (2006), Abstract;
Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity: R.H. Porter, et al.; J. Pharmacol. Exp. Ther. 315, 711 (2005), Abstract;
In vitro and in vivo metabolism of the antianxiolytic agent fenobam in the rat: W.N. Wu, et al.; J. Pharm. Sci. 84, 185 (1995), Abstract;
Novel non-benzodiazepine anxiolytics: M.E. Goldberg, et al.; Neuropharmacology 22, 1499 (1983), Abstract;

Related Products

MPEP . hydrochloride 

mGluR5 antagonist
96206-92-7, ≥99% | Print as PDF
 
ALX-550-368-M005 5 mg 48.00 USD
 
ALX-550-368-M025 25 mg 199.00 USD
Do you need bulk/larger quantities?
 

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