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Biological Activity:
A unique subtype-selective GABAA receptor positive allosteric modulator (PAM); with a subtype selectivity profile at GABAA receptors of α5 > α3 > α2 > α1. Compared with other subtype-selective ligands, NS11394 is unique in having superior efficacy at GABAA-α3 receptors while maintaining low efficacy at GABAA-α1 receptors, which might be attributed for its significantly reduced side effect profile in rat.
References: online
NR Mirza, et al, NS11394 [3'-[5-(1-Hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile], a Unique Subtype-Selective GABAA Receptor Positive Allosteric Modulator: In Vitro Actions, Pharmacokinetic Properties and in Vivo Anxiolytic Efficacy. J. Pharmacol. Exp. Ther. 2008, 327, 954-968.
G. Munro et al. Comparison of the Novel Subtype-Selective GABAA 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. 2008, 327, 969-981.
Chemical Name: 3'-[5-(1-Hydroxy-1-methyl-ethyl)-benzoimidazol-1-yl]-biphenyl-2-carbonitrile
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