MedChemExpress LLC (MCE)

MedChemExpress - Model Fenobam - 57653-26-6

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

Fenobam

MCE China：Fenobam

Brand：MedChemExpress (MCE)

Cat. No.HY-101478

CAS：57653-26-6

Purity：99.0%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

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

In Vitro：Fenobam (300 μM; 72 h) significantly inhibits proliferation and induces apoptosis in LM7 cells[2].

In Vivo：Fenobam (30-60 mg/kg; p.o.; 3 times a week) significantly inhibits self-administration behavior in rats[3].

IC50 & Target：mGluR5 84 nM (IC50) rat mGluR5 54 nM (Kd) human mGluR5 31 nM (Kd)

References：

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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