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

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.

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AMPAR modulator-12

AMPAR modulator-12 Chemical Structure

CAS No. : 2163787-60-6

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AMPAR modulator-12 Related Antibodies

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AMPA Receptor NMDA Receptor Kainate Receptor

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NOX1 NOX2 NOX4 NOX5 DUOX1

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Description

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

 

In Vitro

AMPAR modulator-12 (compound K-4) (100 μM; 20-30 min post-treatment) enhances AMPA receptor-mediated evoked excitatory postsynaptic currents (EPSCs) in hippocampal CA1 pyramidal neurons, resulting in a significant increase in current amplitude relative to baseline levels[1].
AMPAR modulator-12 (0.1 μM) enhances AMPA receptor-mediated evoked excitatory postsynaptic currents in layer 2/3 pyramidal neurons of the barrel cortex[1].

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

AMPAR modulator-12 Related Antibodies
In Vivo

AMPAR modulator-12 (1 mg/kg; intravenous injection; 7 days) exerts rapid, AMPAR-dependent antidepressant-like effects in WKY rats[1].
AMPAR modulator-12 (1 mg/kg; intravenous injection; single administration) exerts rapid antidepressant-like effects in rats with chronic restraint stress-induced depression model[1].

MedChemExpress (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.
Molecular Weight

444.52

Formula

C19H22F2N2O4S2
CAS No.
SMILES

CN(C(COC1=C(C=C(C=C1F)SCCN(S(=O)(C2=CC=CC=C2)=O)C)F)=O)C
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Purity & Documentation
References
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AMPAR modulator-12 Related Classifications

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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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