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mGluR5 antagonist
ALX-550-413-M005 5 mg 88.00 USD
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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 Details

Purity:≥98% (1H-NMR)
Identity:Determined by NMR.
Appearance:Off-white to pale orange solid.
Solubility:Soluble in DMSO or methanol.
Shipping:Ambient Temperature
Long Term Storage:+4°C
Regulatory Status:RUO - Research Use Only
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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;

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MPEP . hydrochloride 

mGluR5 antagonist
96206-92-7, ≥99% | Print as PDF
ALX-550-368-M005 5 mg 61.00 USD
ALX-550-368-M025 25 mg 262.00 USD
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