F0430
Fenobam
≥98% (HPLC), solid
别名:
N-(3-Chlorophenyl)-N′-(4,5-dihydro-1-methyl-4-oxo-1H-imidazole-2-yl)urea
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关于此项目
经验公式（希尔记法）:
C11H11ClN4O2
化学文摘社编号:
分子量:
266.68
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI
1S/C11H11ClN4O2/c1-16-6-9(17)14-10(16)15-11(18)13-8-4-2-3-7(12)5-8/h2-5H,6H2,1H3,(H2,13,14,15,17,18)
SMILES string
CN1CC(=O)N=C1NC(=O)Nc2cccc(Cl)c2
InChI key
DWPQODZAOSWNHB-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
solid
color
white
solubility
DMSO: >20 mg/mL
originator
Johnson & Johnson
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Fenobam is a potent, selective, noncompetitive glutamate mGluR5 receptor antagonist. Fenobam displays inverse agonist properties; blocks mGluR5 constitutive activity in vitro (IC50 = 87 nM, slightly weaker than MPEP). Fenobam 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. Fenobam belongs to a structurally different class than MPEP; devoid of GABAergic activity and thus typical benzodiazepine-like side effects; displays anxiolytic activity.
Potent, selective, noncompetitive metabotropic glutamate receptor antagonist (mGluR5). Displays anxiolytic activity.
Features and Benefits
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
This compound is featured on the Glutamate Receptors (G Protein Family) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges
法规信息
新产品
此项目有
Daniella Rylander et al.
Neurobiology of disease, 39(3), 352-361 (2010-05-11)
L-DOPA remains the gold-standard treatment for Parkinson's disease but causes motor fluctuations and dyskinesia. Metabotropic glutamate receptor type 5 (mGluR5) has been proposed as a target for antidyskinetic therapies. Here, we evaluate the effects of fenobam, a noncompetitive mGluR5 antagonist
Treatment of anxiety using fenobam (a nonbenzodiazepine) in a double-blind standard (diazepam) placebo-controlled study.
J C Pecknold et al.
Journal of clinical psychopharmacology, 2(2), 129-133 (1982-04-01)
E Berry-Kravis et al.
Journal of medical genetics, 46(4), 266-271 (2009-01-08)
A pilot open label, single dose trial of fenobam, an mGluR5 antagonist, was conducted to provide an initial evaluation of safety and pharmacokinetics in adult males and females with fragile X syndrome (FXS). Twelve subjects, recruited from two fragile X
W N Wu et al.
Journal of pharmaceutical sciences, 84(2), 185-189 (1995-02-01)
Fenobam [(Fn); N-(3-chlorophenyl)-N-(4,5-dihydro-1-methyl-4-oxo-1H-imidazole-2-yl)urea] sulfate is a novel agent with potent anxiolytic activity in rats. [14C]Fn sulfate was administered as an oral solution (250 mg/kg) to male Wistar rats, and 52% of the administered dose was excreted in urine (0-5 days).
Michael C Montana et al.
The Journal of pharmacology and experimental therapeutics, 330(3), 834-843 (2009-06-12)
Metabotropic glutamate receptor subtype 5 (mGlu5) has been demonstrated to play a role in the modulation of numerous nociceptive modalities. When administered via peripheral, intrathecal, or systemic routes, mGlu5 antagonists have analgesic properties in a variety of preclinical pain models.
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