NMDAR antagonist 1
产品说明书
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同义名 : | - |
| CAS号 : | 2220162-06-9 | |
| 货号 : | A1155096 | |
| 分子式 : | C20H20BrN3O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 414.3 | |
| MDL号 : | MFCD32173677 | |
| 存储条件： |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : | - |
| 生物活性 | |||
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| 描述 | The N-methyl-D-aspartate receptors (NMDARs) are ionotropic glutamate (iGlu) receptors essential for glutamate excitotoxicity. They play important roles in synaptic plasticity and cell survival. NMDAR antagonist 1 is a potent, orally bioavailable NMDAR antagonist. The viability of SH-SY5Y cells treated with 0.1, 1, 10, and 100 µM NMDAR antagonist 1 was 75.8%, 80.0%, 84.4%, and 78.6%, respectively. NMDAR antagonist 1 at a concentration of 10 μM inhibited NMDA (2 nM)-induced influx of Ca2+ in SH-SY5Y cells. It also suppressed the upregulation of NR2B and increased p-ERK1/2 expression. NMDAR antagonist 1 exhibited high metabolic stability with a clearance rate of 46.3 μL/min/mg in human liver microsomes[1]. | ||
| 作用机制 | NMDAR antagonist 1 is a NR2B-selective NMDAR antagonist. It docks at the NR1-NR2B subunit interface[1]. | ||
| 实验方案 | |||
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| 1mg | 5mg | 10mg | |
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1 mM 5 mM 10 mM |
2.41mL 0.48mL 0.24mL |
12.07mL 2.41mL 1.21mL |
24.14mL 4.83mL 2.41mL |
| 参考文献 |
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