2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. 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.

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GABAA receptor modulator-13

GABAA receptor modulator-13 Chemical Structure

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GABAA receptor modulator-13 Related Antibodies

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Description

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[1].

In Vitro

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.

GABAA receptor modulator-13 Related Antibodies
Parmacokinetics
Species Dose Route T1/2 (Elimination)
Mice[1] 10 mg/kg p.o. 1.25 h
In Vivo

GABAA receptor modulator-13 (10 mg/kg; p.o.; single dose) demonstrates measurable brain penetration in male CD-1 mice following a single 10 mg/kg peroral dose, with a brain-plasma ratio of 0.26 ± 0.042 at Cmax, and is well-tolerated at this dose[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: CD-1 (male)[1]
Dosage: 10 mg/kg
Administration: p.o.; single dose
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.
Molecular Weight

364.83

Formula

C20H17ClN4O
SMILES

O=C(C1=CC=C(C=C1)Cl)NC2=C(N=C3C=CC(C)=CN32)C4=CC=CN4C
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Room temperature in continental US; may vary elsewhere.
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Purity & Documentation
References
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GABAA receptor modulator-13 Related Classifications

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Help & FAQs
  • 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:

GABAA receptor modulator-13GABAA receptor modulator13GABAA receptor modulator 13GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorα4β1δ GABAA receptor modulatorneurodevelopmental disordersepilepsyCD-1 mice
Inhibitorinhibitorinhibit

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