GABAA receptor modulator-13
GABAA receptor modulator-13 is an orally active, blood-brain barrier-permeable α4β1δ GABAA receptor modulator (IC50 = 9.02 μM). GABAA receptor modulator-13 reduces GABA-induced currents, impairs the stability of the transmembrane domain M2-M3 loop of α4β1δ GABAA receptors, and exhibits selectivity for γ2-containing GABAA receptor subtypes and α6β3δ GABAA receptor subtypes. GABAA receptor modulator-13 is applicable to the research of nervous system diseases with altered tonic inhibition, such as neurodevelopmental disorders and epilepsy.
For research use only. We do not sell to patients.
- Formula: C20H17ClN4O
- Molecular Weight:364.83
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
GABAA receptor modulator-13 (1-30 μM; 10 s preapplication, followed by 5 s coapplication with 1 μM GABA) acts as a negative allosteric modulator at human recombinant α4β1δ GABAₐ receptors with an IC50 of 9.02 μM[1].
GABAA receptor modulator-13 (1-30 μM; 10 s preapplication, followed by 5 s coapplication with 1 μM GABA) concentration-dependently inhibits GABA-induced currents at human recombinant α4(T300I)β1δ and α4β1δ(L260V) gain-of-function GABAₐ receptors, with significant effects seen at ≥10 μM and ≥3 μM, respectively[1].
GABAA receptor modulator-13 (10 μM; 5 s coapplication with 1 μM GABA) significantly accelerates the decay of GABA-induced currents at human recombinant α4β1δ GABAₐ receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | T1/2 (Elimination) |
|---|---|---|---|
| Mice[1] | 10 mg/kg | p.o. | 1.25 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 (male)[1]
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Dosage:10 mg/kg
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Administration:p.o.; single dose
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Result:Reached a brain concentration of 97 ng/g and plasma concentration of 3742 ng/mL at 0.5 hours (Cmax).
Resulted in a brain-plasma ratio of 0.26 and an unbound partition coefficient (Kp,uu) of 0.22.
Exhibited a plasma half-life of 1.25 hours.
Showed no gross abnormalities or signs of discomfort in mice.
Chemical Information
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Molecular Weight 364.83
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Formula C20H17ClN4O
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SMILES
O=C(C1=CC=C(C=C1)Cl)NC2=C(N=C3C=CC(C)=CN32)C4=CC=CN4C
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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-13 Related Classifications
HY-181552 Related Classifications
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