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