| 产品描述： | PEAQX (NVP-AAM077) tetrasodium hydrate is a potent, selective and orally active NMDA antagonist, with IC50 values of 270 nM and 29600 nM for hNMDAR 1A/2B and hNMDAR 1A/2B, respectively |
| 靶点： |
NMDA Receptor;Apoptosis; NMDAR; iGluR |
| 体外研究： |
PEAQX (3 μM) 产生类似的 caspase-3 激活，而 NVP-AAM007 的效力大约高出三倍 |
| 体内研究： |
亚慢性给药后，PEAQX (10-40 mg/kg) 以剂量依赖性方式增加皮质 caspase-3 活性。 与盐水预处理 相比, PEAQX（10 和 20 mg/kg）对 PCP 攻击（PN28-35 上 4 mg/kg）的反应增强了运动活性。 PEAQX (10 mg/kg，腹腔注射) 拮抗 PRE084 对 CaMKIV-TORC1-CREB 和 BDNF 的影响，即使是学习和记忆障碍。 Animal Model: Timed, day 14 pregnant female Sprague-Dawley rats. Dosage: 10, 20 or 40 mg/kg. Administration: S.C. Result: Showed a sensitized locomotor response to PCP challenge on PN28-35. Animal Model: Timed, day 14 pregnant female Sprague-Dawley rats. Dosage: 4 mg/kg. Administration: I.P. Result: Did not significantly increase locomotor activity in rats treated sub-chronically with PEAQX on PN7, 9 and 11. Animal Model: 11-week old C57BL/6 mice. Dosage: 10 mg/kg. Administration: IP. Result: Reversed the effect of PRE084 (F3,78 = 10.446, p<0.01). |
| 参考文献： |
1. Auberson YP, et al. 5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonists with a preference for the human 1A/2A, rather than 1A/2B receptor composition. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1099-102. 2. Anastasio NC, et al. Differential role of N-methyl-D-aspartate receptor subunits 2A and 2B in mediating phencyclidine-induced perinatal neuronal apoptosis and behavioral deficits. Neuroscience. 2009 Nov 10;163(4):1181-91. 3. Qian Xu, et al. Sigma-1 receptor in brain ischemia/reperfusion: Possible role in the NR2A-induced pathway to regulate brain-derived neurotrophic factor. J Neurol Sci. 2017 May 15;376:166-175. |
| 溶解性： |
Soluble in H2O |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.202 ml |
11.008 ml |
22.016 ml |
| 5 mM |
0.44 ml |
2.202 ml |
4.403 ml |
| 10 mM |
0.22 ml |
1.101 ml |
2.202 ml |
| 50 mM |
0.044 ml |
0.22 ml |
0.44 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京