2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NMDAR blocker 1

NMDAR blocker 1 是一种 NMDA 受体通道阻滞剂，其 IC50 为 5.0 μM。NMDAR blocker 1 具有快速的开关阻滞动力学特征和强电压依赖性，且不与谷氨酸或甘氨酸竞争结合位点。NMDAR blocker 1 可阻止谷氨酸/NMDA 诱导的细胞内 Ca2+超载，调控谷氨酸-一氧化氮-cGMP (glutamate-nitric oxide-cGMP) 通路。NMDAR blocker 1 可在体外抑制培养的小脑和海马神经元的兴奋性毒性神经退行性变。NMDAR blocker 1 可减轻高氨血症诱导的兴奋性毒性小鼠模型中的兴奋性毒性损伤。NMDAR blocker 1 可用于神经退行性疾病的研究。

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NMDAR blocker 1

NMDAR blocker 1 Chemical Structure

CAS No. : 76991-05-4

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NMDAR blocker 1 相关抗体

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases[1].

IC50 & Target[1]

NMDA Receptor

 

体外研究
(In Vitro)

NMDAR blocker 1 (5-500 μM) 可高效且选择性地抑制非洲爪蟾 (Xenopus laevis) 卵母细胞中大鼠 NR1/NR2A NMDA 受体通道的活性，其 IC50 为 5.0 ± 0.2 μM[1]。
NMDAR blocker 1 (0.1-100 μM; 4 h) 可保护原代大鼠小脑和海马神经元培养物免受兴奋性毒性死亡，在 30 μM 浓度下小脑神经元的存活率最高可达 85 ± 6%[1]。
NMDAR blocker 1 (0.01-30 μM; 5 min) 可剂量依赖性地抑制原代大鼠小脑神经元中 NMDA 诱导的 cGMP 生成[1]。
NMDAR blocker 1 (0.01-100 μM; 10 min) 可强效阻断原代大鼠小脑神经元中 NMDA 诱导的细胞内 Ca2+ 超载，在 100 μM 浓度下可完全抑制[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

NMDAR blocker 1 相关抗体:
体内研究
(In Vivo)

NMDAR blocker 1 (Compound N20C) (5-50 μg/g；腹腔注射；单次给药) 可对雄性瑞士小鼠因急性氨诱导的兴奋性毒性提供剂量依赖性的体内神经保护作用[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ammonia-induced Swiss mice (male, 25-35 g)[1]
Dosage: 5 μg/g; 10 μg/g; 30 μg/g; 50 μg/g
Administration: i.p.; single dose
Result: Increased survival rate.
Caused no conspicuous behavioral or motor deficits in treated animals.
分子量

268.36

Formula

C17H20N2O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NMDAR blocker 1 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NMDAR blocker 176991-05-4NMDAR blocker1NMDAR blocker-1iGluRIonotropic glutamate receptorsGluR1hippocampal neuronsvoltage-dependent Ca2+ channelsXenopus laevis oocytescerebellar neuronsrat NMDA receptorsNMDA receptorsInhibitorinhibitorinhibit

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