Formulation: A crystalline solid
Formal Name: 3'-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-[1,1'-biphenyl]-2-carbonitrile
Purity: ≥98%
Formula Markup: C23H19N3O
Formula Weight: 353,4
Shelf life (days): 1460
CAS Number: 951650-22-9
Notes: NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes).{36345} It is 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). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits α3 and α5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Item No. ISO60177). In vivo, NS 11394 inhibits the binding of [3H]flunitrazepam to benzodiazepine receptors in the forebrain of mice and rats, with respective EC50 values of 0.38 and 1.3 mg/kg at 30 minutes and 0.49 and 0.69 mg/kg at 120 minutes following oral administration. NS 11394 (1-30 mg/kg) attenuates spontaneous nociceptive behaviors to formalin and capsaicin (Item No. 92350) injections in a rat model of neuropathic pain.{36346}
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