| 产品描述: | 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 |
| 靶点: |
GABA Receptor;GABAReceptor |
| 体内研究: |
NS11394 (1-120 mg/kg) selectively attenuates injury-induced nociceptive behaviors in the formalin test. NS11394 (1–10 mg/kg) markedly attenuates the deficit in hindpaw weight bearing [F(4,61) = 7.569, p < 0.001] in CFA rats. Animal Model: Adult male Sprague-Dawley rats. Dosage: 1-120 mg/kg. Administration: Orally. Result: Significantly attenuated motor function compared with corresponding vehicle responses.Significantly reduced flinching behavior during interphase [F(3,30) = 4.139, p < 0.05] and the second phase [F(3,30) = 11.033, p < 0.001] of the formalin test compared with vehicle treatment indicative of a selective effect on injury-induced nociceptive transmission. |
| 参考文献: |
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 Efficacy 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 Models of Inflammatory and Neuropathic Pain 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. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.83 ml |
14.148 ml |
28.295 ml |
| 5 mM |
0.566 ml |
2.83 ml |
5.659 ml |
| 10 mM |
0.283 ml |
1.415 ml |
2.83 ml |
| 50 mM |
0.057 ml |
0.283 ml |
0.566 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |