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NMDAR antagonist 1

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Chemical Structure| 2220162-06-9 同义名 : -
CAS号 : 2220162-06-9
货号 : A1155096
分子式 : C20H20BrN3O2
纯度 : 99%+
分子量 : 414.296
MDL号 : MFCD32173677
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
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
1mg 5mg 10mg

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

[1]Zhang L, Zhao Y, Wang J, Yang D, Zhao C, Wang C, Ma C, Cheng M. Design, synthesis and bioevaluation of 1,2,3,9-tetrahydropyrrolo[2,1-b]quinazoline-1-carboxylic acid derivatives as potent neuroprotective agents. Eur J Med Chem. 2018 May 10;151:27-38. doi: 10.1016/j.ejmech.2018.03.052