| Identification | Back Directory | [Name]
3-(3-chlorophenyl)-1-(1-methyl-4-oxo-5H-imidazol-2-yl)urea hydrate | [CAS]
63540-28-3 | [Synonyms]
Unii-07o6708m02
Fenobam (hydrate)
Fenobam [usan:inn]
3-(3-chlorophenyl)-1-(1-methyl-4-oxo-5H-imidazol-2-yl)urea hydrate | [Molecular Formula]
C11H13ClN4O3 | [MOL File]
63540-28-3.mol |
| Hazard Information | Back Directory | [Description]
Fenobam is a noncompetitive antagonist and inverse agonist of metabotropic glutamate receptor 5 (mGluR5) that binds to an allosteric site. It inhibits intracellular calcium mobilization induced by the glutamate analog quisqualate in HEK293 cells expressing the human receptor (IC50 = 58 nM) and inhibits basal activity of mGluR5 in a cell-based assay (IC50 = 84 nM). Fenobam (10 and 30 mg/kg) reduces stress-induced hyperthermia in mice and increases drinking time in the Vogel conflict test in rats when administered at a dose of 30 mg/kg, indicating anxiolytic-like activity. It induces analgesia in the formalin test in mice when administered at a dose of 30 mg/kg. | [Uses]
Sedative-hypnotic. | [in vivo]
Fenobam hydrate (30-60 mg/kg; p.o.; 3 times a week) significantly inhibits self-administration behavior in rats[3]. | Animal Model: | Male Long-Evans rats (250-300 g)[3]. | | Dosage: | 30-60 mg/kg | | Administration: | Oral administration; 3 times a week. | | Result: | Inhibited self-administration. |
| [IC 50]
mGluR5: 84 nM (IC50); human mGluR5: 31 nM (Kd); rat mGluR5: 54 nM (Kd) | [References]
[1] RICHARD H P PORTER. Fenobam: a clinically validated nonbenzodiazepine anxiolytic is a potent, selective, and noncompetitive mGlu5 receptor antagonist with inverse agonist activity.[J]. Journal of Pharmacology and Experimental Therapeutics, 2005, 315 2: 711-721. DOI: 10.1124/jpet.105.089839
[2] MICHAEL C MONTANA. Metabotropic glutamate receptor 5 antagonism with fenobam: examination of analgesic tolerance and side effect profile in mice.[J]. ACS Catalysis , 2011: 1239-1250. DOI: 10.1097/aln.0b013e318238c051 |
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