Description
A positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM); selective for GABAA receptors containing α1, α2, α3, or α5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α4 or α6 subunits (Kis = 324 or 1,009 nM, respectively); modulator of GABA receptors containing subunits α3 and α5 with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam; inhibits [3H]flunitrazepam binding to benzodiazepine receptors in mouse and rat forebrain in vivo (EC50s = 0.38 and 1.3 mg/kg, respectively, at 30 minutes and 0.49 and 0.69 mg/kg, respectively, at 120 minutes following oral administration); attenuates spontaneous nociceptive behaviors in a rat model of neuropathic pain when administered at doses of 1-30 mg/kg
Formal name: 3′-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-[1,1′-biphenyl]-2-carbonitrile
Synonyms:
Molecular weight: 353.4
CAS: 951650-22-9
Purity: ≥98%
Formulation: A crystalline solid
Product Type|Biochemicals|Ion Channel Modulation|Activators||Research Area|Neuroscience|Pain Research
