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Biological Activity for Fenobam
Fenobam is a potent and selective non-competitive mGlu5 negative allosteric modulator (NAM) that also displays inverse agonist properties; blocks mGlu5 constitutive activity in vitro (IC50 = 87 nM). Acts at an allosteric modulatory site shared with MPEP and binds the mGlu5 receptor with Kd values of 54 and 31 nM for rat and human receptors respectively. Displays anxiolytic activity following oral administration in vivo; also exhibits analgesic properties.
Compound Libraries for Fenobam
Technical Data for Fenobam
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Fenobam
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Fenobam
The following data is based on the product molecular weight 266.69. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.75 mL||18.75 mL||37.5 mL|
|5 mM||0.75 mL||3.75 mL||7.5 mL|
|10 mM||0.37 mL||1.87 mL||3.75 mL|
|50 mM||0.07 mL||0.37 mL||0.75 mL|
References for Fenobam
References are publications that support the biological activity of the product.
Porter et al (2005) Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity. J.Pharmacol.Exp.Ther. 315 711 PMID: 16040814
Montana et al (2009) The metabotropic glutamate receptor subtype 5 antagonist fenobam is analgesic and has improved in vivo selectivity compared with the prototypical antagonist 2-methyl-6-(phenylethynyl)-pyridine. J.Pharmacol.Exp.Ther. 330 834 PMID: 19515968
Porter et al (2005) Description of a clinically validated anxiolytic with mGlu5 antagonist properties. Neuropharmacology 49 267
Kufahl et al (2013) Positive or negative allosteric modulation of metabotropic glutamate receptor 5 (mGluR5) does not alter expression of behavioral sensitization to methamphetamine F1000Res. 1 10.12688/f1000resear PMID: 24358885
Liu et al (2018) Orthosteric and allosteric action of the C5a receptor antagonists Nature Structural & Molecular Biology 25 472 PMID: 29867214
If you know of a relevant reference for Fenobam, please let us know.
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Keywords: Fenobam, Fenobam supplier, Potent, selective, mGlu5, antagonist, mGluR5, antagonists, Group, I, Receptors, Glutamate, Metabotropic, (Metabotropic), 2386, Tocris Bioscience
1 Citation for Fenobam
Citations are publications that use Tocris products. Selected citations for Fenobam include:
Crock et al (2012) Metabotropic glutamate receptor 5 (mGluR5) regulates bladder nociception. Mol Pain 8 20 PMID: 22449017
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Huntington's Disease PosterUpdated
Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.