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

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GABAA receptor modulator-10

GABAA receptor modulator-10 Chemical Structure

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Description

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[1].

IC50 & Target[1]

α1β2γ2 GABAA receptor

 

In Vitro

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 Related Antibodies
In Vivo

GABAA receptor modulator-10 (Compound 10) (10 μM, exposed for 3 h before PTZ treatment) reduces the total movement distance of 6-day post-fertilization (dpf) AB wild-type zebrafish[1].
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.

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]
Dosage: 0.3 mg/kg, 1 mg/kg, 10 mg/kg, 30 mg/kg
Administration: p.o., 1 h before PTZ injection
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.
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]
Dosage: 30 mg/kg
Administration: p.o., 30 min before KA injection
Result: Attenuated seizure severity.
Showed comparable effect to diazepam.
Molecular Weight

395.82

Formula

C20H15ClFN5O
SMILES

O=C(NC1=CC=C(Cl)C=C1)C2=CC(C3=C4N=CN(CC)C4=NC=N3)=CC=C2F
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Room temperature in continental US; may vary elsewhere.
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GABAA receptor modulator-10 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-10GABAA receptor modulator10GABAA receptor modulator 10GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid Receptorepilepsyα1β2γ2 GABAA receptorInhibitorinhibitorinhibit

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