AMPA receptor modulator-12
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.
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- Formel: C25H24F2N2O3S
- Molecular Weight:470.53
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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- Reinheit & Dokumentation
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
AMPA Receptor |
In Vitro
AMPA receptor modulator-12 (Compound B1) (10-9-10-3 M; 20 min) exhibits moderate binding affinity for the human dopamine transporter with a Kd of 1.57 μM[1].
AMPA receptor modulator-12 (50 μM-1 mM) concentration-dependently enhancing glutamate-induced peak currents and delaying channel deactivation in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
AMPA receptor modulator-12 (0.2 mmol/kg; i.g.; daily; 5 days) in a pentobarbital-induced sleep mouse model, significantly prolonging sleep latency, reducing sleep onset rate, and shortening sleep duration[1].
AMPA receptor modulator-12 (0.2 mmol/kg; i.g.; daily; 5 days) exhibits significant anti-fatigue activity in mice, prolonging weight-loaded forced swimming time and rotarod endurance and reduces exercise-induced accumulation of fatigue-related metabolic waste products[1].
AMPA receptor modulator-12 (0.2 mmol/kg; p.o.; at 24, 48, and 72 hours during sleep deprivation) effectively reverses behavioral deficits induced by 72 hours of acute sleep deprivation in mice, restoring locomotor and exploratory activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pentobarbital-induced sleep mouse model (male, 3-8 weeks old, 18-22 g)[1]
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Dosage:0.2 mmol/kg
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Administration:I.g.,; daily; 5 days
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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.
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Animal Model:Acute sleep deprivation-induced behavioral deficit in mice (male, 3-8 weeks old, 18-22 g)[1]
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Dosage:0.2 mmol/kg
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Administration:I.g.; at 24, 48, and 72 hours during sleep deprivation
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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.
Chemical Information
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Molecular Weight 470.53
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Formel C25H24F2N2O3S
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SMILES
O=C(NCCCNC(CS(C(C1=CC=C(F)C=C1)C2=CC=C(F)C=C2)=O)=O)C3=CC=CC=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Protocol for Open Field Test (OF)
The Open Field Test is a rodent behavioral assay that measures spontaneous locomotion, exploratory behavior, and anxiety-like behavior when an animal is placed in a novel open arena. The main readouts are total distance traveled, movement time, velocity, center-zone entries, center-zone time, peripheral-zone time, and thigmotaxis. The assay is based on the conflict between exploration of a novel environment and avoidance of exposed open areas; higher center exploration is commonly interpreted as lower anxiety-like behavior, whereas increased wall-following or peripheral occupancy is interpreted as higher anxiety-like behavior.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
AMPA receptor modulator-12 Related Classifications
HY-183324 Related Classifications
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Keywords
- AMPA receptor modulator-12
- AMPA receptor modulator12
- AMPA receptor modulator 12
- iGluR
- Dopamine Transporter
- GluA1/GluA2
- HEK293T cells
- glutamate
- hippocampal neuronal damage
- dopamine transporter
- AMPA receptor
- fatigue-related conditions
- narcolepsy
- acute sleep deprivation
- pentobarbital-induced sleep mouse model
- Inhibitor
- inhibitor
- inhibit