GABAA receptor modulator-10
GABAA receptor modulator-10 is an orally active, potent positive allosteric modulator (PAM) of the α1β2γ2 GABAA receptor with favorable blood-brain barrier (BBB) penetration. GABAA receptor modulator-10 enhances α1β2γ2 GABAA receptor function and potentiates GABA-evoked currents. GABAA receptor modulator-10 demonstrates potent antiepileptic efficacy in both the Pentetrazol (PTZ)- and Kainic Acid (KA) (HY-N2309)-induced mice epilepsy models. GABAA receptor modulator-10 can be used for the study of epilepsy.
For research use only. We do not sell to patients.
- Formula: C20H15ClFN5O
- Molecular Weight:395.82
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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α1β2γ2 GABAA receptor |
GABAA receptor modulator-10 (Compound 10) (10 μM) enhances α1β2γ2 GABAA receptor function in HEK293T cells overexpressing α1β2γ2 GABAA receptor via MQAE-based fluorescence assay[1].
GABAA receptor modulator-10 (0.1-100 μM) potentiates GABA-evoked currents in a concentration-dependent manner in HEK293T cells overexpressing α1β2γ2 GABAA receptor (EC50 = 1.99 μM and Emax = 80.1%) via patch-clamp assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GABAA receptor modulator-10(0.3-30 mg/kg, p.o., 1 h before PTZ injection) prolongs the latency of stage I seizures and stage III seizures shortens stage III seizure duration, and prevents stage V seizure in PTZ-induced mouse epilepsy model[1].
GABAA receptor modulator-10 (30 mg/kg, p.o., 30 min before KA injection) attenuates seizure severity, reduces mortality in KA-induced mouse temporal lobe epilepsy model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:PTZ-induced mouse epilepsy model: Male KM mice (18-20 g) were were subcutaneously injected with 85 mg/kg PTZ (dissolved in saline) to induce seizures[1]
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Dosage:0.3 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:p.o., 1 h before PTZ injection
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Result:Prolonged the latency of stage I seizures by 1.21-, 0.96-, 1.53-, and 2.20-fold, and stage III seizures by 1.02-, 1.03-, 1.22-, and 1.45-fold, respectively.
Shortened the duration of stage III seizures.
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Animal Model:KA-induced mouse temporal lobe epilepsy (TLE) model: Male C57B6/J mice (18-20 g) were intraperitoneally injected with 30 mg/kg kainic acid (KA, dissolved in saline) to induce TLE[1]
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Dosage:30 mg/kg
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Administration:p.o., 30 min before KA injection
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Result:Attenuated seizure severity.
Showed comparable effect to diazepam.
Chemical Information
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Molecular Weight 395.82
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Formula C20H15ClFN5O
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SMILES
O=C(NC1=CC=C(Cl)C=C1)C2=CC(C3=C4N=CN(CC)C4=NC=N3)=CC=C2F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GABAA receptor modulator-10 Related Classifications
HY-175670 Related Classifications
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