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Fenobam (hydrate)

Fenobam hydrate is a selective and orally active mGluR5 antagonist (IC50=84 nM) that can penetrate the blood-brain barrier. Fenobam hydrate shows the Kd values of 54 nM and 31 nM on rat and human recombinant mGlu5 receptors, respectively. Fenobam hydrate has anxiolytic activity, inhibits self-administration behavior in rat, and induces apoptosis in cancer cells. Fenobam hydrate can be used for research on neurological diseases, cancer and drug addiction[1][2][3].

Product Specifications

CAS Number

63540-28-3

UNSPSC

12352005

Target

Apoptosis; mGluR

Type

Reference compound

Related Pathways

Apoptosis; GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/fenobam-hydrate.html

Solubility

10 mM in DMSO

Smiles

O=C(NC1=NC(CN1C)=O)NC2=CC=CC(Cl)=C2.O

Molecular Formula

C11H13ClN4O3

Molecular Weight

284.70

References & Citations

[1]Porter RH, et al. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J Pharmacol Exp Ther. 2005 Nov;315 (2) :711-21.|[2]Liao S, et al. Osteosarcoma cell proliferation and survival requires mGluR5 receptor activity and is blocked by Riluzole. PLoS One. 2017 Feb 23;12 (2) :e0171256.|[3]Keck TM, et al. Fenobam sulfate inhibits cocaine-taking and cocaine-seeking behavior in rats: implications for addiction treatment in humans. Psychopharmacology (Berl) . 2013;229 (2) :253-265.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

MGluR5

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