MedChemExpress - Model Fenobam hydrate - 63540-28-3
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].MCE products for research use only. We do not sell to patients.
Fenobam hydrate
MCE China：Fenobam hydrate
Brand：MedChemExpress (MCE)
Cat. No.HY-101478A
CAS：63540-28-3
Storage：Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：Fenobam hydrate (300 μM; 72 h) significantly inhibits proliferation and induces apoptosis in LM7 cells[2].
In Vivo：Fenobam hydrate (30-60 mg/kg; p.o.; 3 times a week) significantly inhibits self-administration behavior in rats[3].
IC50 & Target：mGluR5 84 nM (IC50) human mGluR5 31 nM (Kd) rat mGluR5 54 nM (Kd)
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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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