2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR Dopamine Transporter
  4. AMPA receptor modulator-12

AMPA receptor modulator-12 是一种具有口服活性的 AMPA 受体正向变构调节剂。AMPA receptor modulator-12 对人多巴胺转运体 (dopamine transporter) 也表现出中等结合亲和力，其 Kd 值为 1.57 μM。AMPA receptor modulator-12 可增强 AMPA 受体介导的离子电流，延迟通道失活。AMPA receptor modulator-12 可延长睡眠潜伏期、缩短睡眠时长、延长强迫游泳时间、提升转棒耐力，并缓解急性睡眠剥夺相关的行为缺陷。AMPA receptor modulator-12 不会增加自发性运动能力。AMPA receptor modulator-12 可用于发作性睡病及疲劳相关病症的研究。

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AMPA receptor modulator-12

AMPA receptor modulator-12 Chemical Structure

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AMPA receptor modulator-12 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

AMPA receptor modulator-12 is an orally acrive AMPA receptor positive allosteric modulator. AMPA receptor modulator-12 also exhibits moderate binding affinity for the human dopamine transporter with a Kd of 1.57 μM. AMPA receptor modulator-12 enhances AMPA receptor-mediated ion currents, delays channel deactivation. AMPA receptor modulator-12 prolongs sleep latency, reduces sleep duration, extends forced swimming time, improves rotarod endurance, and alleviates acute sleep deprivation-related behavioral deficits. AMPA receptor modulator-12 does not increase spontaneous locomotion. AMPA receptor modulator-12 can be used for the research of narcolepsy and fatigue-related conditions[1].

IC50 & Target[1]

AMPA Receptor

 

体外研究
(In Vitro)

AMPA receptor modulator-12 (Compound B1) (10-9-10-3 M; 20 min) 对人多巴胺转运体表现出中等结合亲和力，其 Kd 值为 1.57 μM[1]。
AMPA receptor modulator-12 (50 μM-1 mM) 可浓度依赖性地增强 HEK293T 细胞中谷氨酸诱导的峰值电流并延缓通道失活[1]。

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

AMPA receptor modulator-12 相关抗体:
体内研究
(In Vivo)

AMPA receptor modulator-12 (Compound B1) (0.2 mmol/kg；灌胃；每日 1 次，连续 5 天) 不会影响小鼠的自主运动能力[1]。
AMPA receptor modulator-12 (0.2 mmol/kg；灌胃；每日 1 次，连续 5 天) 在戊巴比妥诱导的睡眠小鼠模型中展现出强效的促觉醒活性，可显著延长睡眠潜伏期、降低入睡率并缩短睡眠时长[1]。
AMPA receptor modulator-12 (0.2 mmol/kg；灌胃；每日一次；连续 5 天) 在小鼠中表现出显著的抗疲劳活性，可延长负重强迫游泳时间和转棒耐力，可减少小鼠运动诱导的疲劳相关代谢废物堆积[1]。
AMPA receptor modulator-12 (0.2 mmol/kg；口服；睡眠剥夺期间的 24、48 和 72 小时给药) 可有效逆转小鼠中 72 小时急性睡眠剥夺诱导的行为缺陷，恢复其自主活动与探究活动[1]。

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

Animal Model: Pentobarbital-induced sleep mouse model (male, 3-8 weeks old, 18-22 g)[1]
Dosage: 0.2 mmol/kg
Administration: I.g.,; daily; 5 days
Result: Prolonged sleep latency significantly compared to the blank control group.
Reduced sleep onset rate to 60%.
Shortened sleep duration markedly compared to both the blank control group and the positive control modafinil group.
Did not cause significant changes in spontaneous locomotor activity relative to the blank control group.
Animal Model: Acute sleep deprivation-induced behavioral deficit in mice (male, 3-8 weeks old, 18-22 g)[1]
Dosage: 0.2 mmol/kg
Administration: I.g.; at 24, 48, and 72 hours during sleep deprivation
Result: Increased total movement time significantly, total travel distance significantly, and center zone movement significantly compared to the sleep-deprived model group, reversing deficits in spontaneous activity and exploratory behavior.
Prevented sleep deprivation-induced hippocampal neuronal necrosis in the CA1 and DG regions, maintaining abundant, regularly aligned, compact neurons without evident degeneration or necrosis, similar to the non-deprived blank control group.
分子量

470.53

Formula

C25H24F2N2O3S
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

AMPA receptor modulator-12 相关分类

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  • 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:

AMPA receptor modulator-12AMPA receptor modulator12AMPA receptor modulator 12iGluRDopamine TransporterIonotropic glutamate receptorsDATSLC6A3GluA1/GluA2HEK293T cellsglutamatehippocampal neuronal damagedopamine transporterAMPA receptorfatigue-related conditionsnarcolepsyacute sleep deprivationpentobarbital-induced sleep mouse modelInhibitorinhibitorinhibit

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