2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR Dopamine Transporter
  4. 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.

For research use only. We do not sell to patients.

AMPA receptor modulator-12

AMPA receptor modulator-12 Chemical Structure

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AMPA receptor modulator-12 Related Antibodies

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Description

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

 

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.

AMPA receptor modulator-12 Related Antibodies
In Vivo

AMPA receptor modulator-12 (Compound B1) (0.2 mmol/kg; i.g.; daily; 5 days) does not affect locomotor activity in mice[1].
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.

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.
Molecular Weight

470.53

Formula

C25H24F2N2O3S
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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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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AMPA receptor modulator-12 Related Classifications

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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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