2. Membrane Transporter/Ion Channel Neuronal Signaling Metabolic Enzyme/Protease
  3. iGluR NADPH Oxidase
  4. AMPAR modulator-12

AMPAR modulator-12 是一种可透过血脑屏障的 AMPAR 正向变构调节剂。AMPAR modulator-12 可降低 NOX-1 表达、增强 AMPAR 介导的电流、促进兴奋性突触后传递并恢复 AMPAR 功能。AMPAR modulator-12 可增强兴奋性和抑制性突触传递、减少戒断后外侧缰核的爆发式放电，并产生快速且持久的类抗抑郁作用。AMPAR modulator-12 可用于抑郁症的研究。

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AMPAR modulator-12

AMPAR modulator-12 Chemical Structure

CAS No. : 2163787-60-6

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AMPAR modulator-12 相关抗体

Top Publications Citing Use of Products

查看 iGluR 亚型特异性产品:

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AMPA Receptor NMDA Receptor Kainate Receptor

查看 NADPH Oxidase 亚型特异性产品:

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NOX1 NOX2 NOX4 NOX5 DUOX1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression[1].

IC50 & Target[1]

AMPA Receptor

 

NOX1

 

体外研究
(In Vitro)

AMPAR modulator-12 (compound K-4) (100 μM; 20-30 min post-treatment) 可增强海马 CA1 锥体神经元中 AMPA 受体介导的诱发兴奋性突触后电流 (EPSCs)，使电流幅度较基线水平显著升高[1]。
AMPAR modulator-12 (0.1 μM) 增强桶状皮层 2/3 层锥体神经元中 AMPA 受体介导的诱发兴奋性突触后电流[1]。

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

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

AMPAR modulator-12 (1 mg/kg；静脉注射；7 天) 在 WKY 大鼠中发挥快速的、AMPAR 依赖性的类抗抑郁作用[1]。
AMPAR modulator-12 (1 mg/kg；静脉注射；单次给药) 在慢性束缚应激诱导的抑郁模型大鼠中发挥快速的类抗抑郁作用[1]。

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

Animal Model: Wistar Kyoto (WKY) rats (male, 5-11 weeks old, congenital depressive phenotype model)[1]
Dosage: 1 mg/kg
Administration: i.v.; single administration; daily for 7 days
Result: Significantly reduced immobility time in the FST, shortened latency to touch and feed in the NSFT, and increased sucrose preference in the SPT at 3 h post-treatment compared to vehicle.
Showed significantly reduced immobility time in the FST on day 8 and day 15 post-withdrawal after 7 days of daily administration; this effect was abolished by co-administration of the AMPAR antagonist GYKI53655.
Significantly increased sucrose preference in the SPT on day 8 and day 15 post-withdrawal, and reduced immobility time in the FST on day 22 post-withdrawal.
Showed no significant differences in locomotor activity compared to vehicle-treated rats.
Significantly restored mEPSC amplitude and increased mEPSC frequency in layer 2/3 pyramidal neurons of the mPFC 30 min post-injection compared to vehicle.
Showed significantly increased mEPSC and mIPSC amplitudes in mPFC pyramidal neurons, and significantly reduced burst firing in lateral habenula (LHb) neurons seven days post-withdrawal from daily administration compared to vehicle controls.
Downregulated Nox1 expression by 2.61-fold compared to ketamine treatment, and by 2.28-fold compared to intact rats in bulk RNA sequencing of mPFC tissue 7 days post-withdrawal.
分子量

444.52

Formula

C19H22F2N2O4S2
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

AMPAR 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:

AMPAR modulator-122163787-60-6AMPAR modulator12AMPAR modulator 12iGluRNADPH OxidaseIonotropic glutamate receptorsNOXWKY ratstreatment-resistant depressionmPFCbarrel cortex Layer 2/3 pyramidal neuronschronic restraint stress-induced depression model ratsWistar ratsNOX-1hippocampal CA1 pyramidal neuronsAMPARLHbInhibitorinhibitorinhibit

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