| Bioactivity | NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties[1][2][3]. | ||||||||||||
| In Vivo | NS11394 (1-120 mg/kg) selectively attenuates injury-induced nociceptive behaviors in the formalin test[2].NS11394 (1–10 mg/kg) markedly attenuates the deficit in hindpaw weight bearing [F(4,61) = 7.569, p < 0.001] in CFA rats[2]. Animal Model: | ||||||||||||
| Name | NS11394 | ||||||||||||
| CAS | 951650-22-9 | ||||||||||||
| Formula | C23H19N3O | ||||||||||||
| Molar Mass | 353.42 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. N. R. 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 Effica [2]. G. Munro, J. A., 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 [3]. Martine Hofmann, et al. Assessment of the effects of NS11394 and L-838417, a2/3 subunit-selective GABAA receptor-positive allosteric modulators, in tests for pain, anxiety, memory and motor function. Behavioural Pharmacology 2012, 23:790–801. |