GABAA receptor agent 7
GABAA receptor agent 7 (compoud 5c) is a potent GABAA receptor positive modulator. GABAA receptor agent 7 shows anticonvulsant activity in vitro and in vivo with low neurotoxicity. GABAA receptor agent 7 has the potential for the research of epilepsy.
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- CAS No.: 2376841-18-6
- Formule: C18H13ClN4O
- Masse moléculaire:336.78
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
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Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
0.2 μM
Compound: 5c
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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 |
3.08 μM
Compound: 5c
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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 |
0.452 μM
Compound: 5c
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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] |
In Vitro
GABAA receptor agent 7 (compoud 5c) shows anticonvulsant activity with an IC50 of 0.452 µM in 4-AP induced hyper-excitability Model[1].
GABAA receptor agent 7 (0.01-100 µM; 0-140 s) increases GABA-induced activation of GABAA1 receptor in a dose-dependent manner with EC50 3.08 µM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
GABAA receptor agent 7 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. 2376841-18-6
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Masse moléculaire 336.78
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Formule C18H13ClN4O
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SMILES
O=C1C=C(CC2=CC=C(Cl)C=C2)N=C3N1NC(C4=CC=CC=C4)=N3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Neurotoxicity Study
This protocol assesses in vitro neurotoxicity by combining neuronal viability, mitochondrial/metabolic activity, neurite outgrowth, and optional neuronal network function readouts. Calcein-AM or resazurin/PrestoBlue readouts estimate viable or metabolically active cells; βIII-tubulin immunofluorescence detects neuronal morphology and neurite networks; TMRE detects mitochondrial membrane potential; and MEA recordings detect functional changes in neuronal network activity.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GABAA receptor agent 7 Related Classifications
HY-146099 Related Classifications
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