GABAA receptor agent 8
GABAA receptor agent 8 (compoud 5e) is a potent GABAA receptor positive modulator. GABAA receptor agent 8 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 8 has the potential for the research of epilepsy.
For research use only. We do not sell to patients.
- CAS No.: 2376841-54-0
- Formula: C19H16N4O
- Molecular Weight:316.36
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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[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
0.24 μM
Compound: 5e
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Positive allosteric modulation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells at 30 uM in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay (Rvb = 0.25 +/- 0.03 uM)
Positive allosteric modulation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells at 30 uM in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay (Rvb = 0.25 +/- 0.03 uM)
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[PMID: 31708184] |
| CHO | EC50 |
12.02 μM
Compound: 5e
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Activation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay
Activation of recombinant human GABA receptor alpha1beta2gamma2 expressed in CHO cells in presence of GABA and measured for 120 secs by FMP dye based FLIPR assay
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[PMID: 31708184] |
| Cortical neurone | IC50 |
0.334 μM
Compound: 5e
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Antiepileptic actvity in C57BL/6 mouse Primary cortical neuron assessed as reduction in 4-AP-induced excitability measured for 8 mins by Fluo-8/AM staining based FLIPR assay
Antiepileptic actvity in C57BL/6 mouse Primary cortical neuron assessed as reduction in 4-AP-induced excitability measured for 8 mins by Fluo-8/AM staining based FLIPR assay
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[PMID: 31708184] |
GABAA receptor agent 8 (compoud 5e) shows anticonvulsant activity with an IC50 of 0.334 µM in 4-AP induced hyper-excitability Model[1].
GABAA receptor agent 8 (0.01-100 µM; 0-140 s) increases GABA-induced activation of GABAA1 receptor in a dose-dependent manner with EC50 12.02 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GABAA receptor agent 8 specifically attenuates PTZ-induced seizures but not MES-induced seizures in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2376841-54-0
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Molecular Weight 316.36
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Formula C19H16N4O
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SMILES
O=C1C=C(CC2=CC=CC=C2)N=C3N1NC(C4=CC=C(C)C=C4)=N3
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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 agent 8 Related Classifications
HY-146100 Related Classifications
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