NS 11394

NS 11394 is an orally bioavailable positive allosteric modulator of the GABAA receptor (Ki = 0.423 nM in rat cortical membranes). It is selective for GABAA receptors containing alpha1, alpha2, alpha3, or alpha5 subunits (Kis = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing alpha4 or alpha6 subunits (Kis = 324 or 1,009 nM, respectively). In X. laevis oocytes, NS 11394 modulates GABA responses via receptors containing the subunits alpha3 and alpha5, with maximal potentiation rates of 52% and 78%, respectively, relative to diazepam (Cay-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 (Cay-92350) injections in a rat model of neuropathic pain.Formal Name: 3'-[5-(1-hydroxy-1-methylethyl)-1H-benzimidazol-1-yl]-[1,1'-biphenyl]-2-carbonitrile. CAS Number: 951650-22-9. Molecular Formula: C23H19N3O. Formula Weight: 353.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 33 mg/ml3, DMSO: 33 mg/ml3, Ethanol: 33 mg/ml3, Ethanol:PBS(pH 7.2) (1:5): 0.16 mg/ml. lambdamax: 251 nm. SMILES: OC(C)(C)C(C=C1)=CC2=C1N(C=N2)C3=CC=CC(C4=C(C#N)C=CC=C4)=C3. InChi Code: InChI=1S/C23H19N3O/c1-23(2,27)18-10-11-22-21(13-18)25-15-26(22)19-8-5-7-16(12-19)20-9-4-3-6-17(20)14-24/h3-13,15,27H,1-2H3. InChi Key: HLKYSQGBIIIQJN-UHFFFAOYSA-N.