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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- CAS 番号: 2163787-60-6
- 分子式: C19H22F2N2O4S2
- 分子量:444.52
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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AMPA Receptor |
NOX1 |
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 (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.
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Animal Model:Wistar Kyoto (WKY) rats (male, 5-11 weeks old, congenital depressive phenotype model)[1]
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Dosage:1 mg/kg
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Administration:i.v.; single administration; daily for 7 days
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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.
化学情報
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CAS 番号 2163787-60-6
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分子量 444.52
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分子式 C19H22F2N2O4S2
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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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
AMPAR modulator-12 関連分類
HY-183101 関連分類
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- AMPAR modulator-12
- 2163787-60-6
- AMPAR modulator12
- AMPAR modulator 12
- iGluR
- NADPH Oxidase
- WKY rats
- treatment-resistant depression
- mPFC
- barrel cortex Layer 2/3 pyramidal neurons
- chronic restraint stress-induced depression model rats
- Wistar rats
- NOX-1
- hippocampal CA1 pyramidal neurons
- AMPAR
- LHb
- Inhibitor
- inhibitor
- inhibit