NS 11394

NS 11394 is an orally bioavailable positive allosteric modulator of the GABA_A receptor (K_i = 0.423 nM in rat cortical membranes).¹ It is selective for GABA_A receptors containing α₁, α₂, α₃, or α₅ subunits (K_is = 0.41, 0.84, 0.497, and 0.119 nM, respectively) over receptors containing α₄ or α₆ subunits (K_is = 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.²

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1. Mirza, N.R., Larsen, J.S., Mathiasen, C., et al. NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a unique subtype-selective GABA_A receptor positive allosteric modulator: In vitro actions, pharmacokinetic properties and in vivo anxiolytic efficacy. J. Pharmacol. Exp. Ther. 327(3), 954-968 (2008).

2. Muro, G., Lopez-Garcia, J.A., Rivera-Arconada, I., et al. Comparison of the novel subtype-selective GABA_A receptor-positive allosteric modulator NS11394 [3'-[5-(1-hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile] with diazepam, zolpidem, bretazenil, and gaboxadol in rat models of inflammatory and neuropathic pain. J. Pharmacol. Exp. Ther. 327(3), 969-981 (2008).