Fenobam

ALX-550-413

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mGluR5 antagonist

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.

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Product Details

Appearance	Off-white to pale orange solid.
CAS	57653-26-6
Couple Target	Metabotropic glutamate receptor
Couple Type	Inhibitor
Formula	C₁₁H₁₁ClN₄O₂
Identity	Determined by NMR.
MW	266.7
Purity	≥98% (1H-NMR)
Solubility	Soluble in DMSO or methanol.

Handling & Storage

Use/Stability	As indicated on product label or CoA when stored as recommended.
Long Term Storage	+4°C
Shipping	Ambient Temperature

Regulatory Status	RUO – Research Use Only

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

ALX-550-368

mGluR5 antagonist

13 citations

Alternative Name	6-Methyl-2-(phenylethynyl)-pyridine . HCl
CAS	96206-92-7
Couple Type	Inhibitor, Ligand
Purity	≥99%

Last modified: May 29, 2024

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Fenobam

ALX-550-413

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