1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. 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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GABAA receptor agent 7 Chemical Structure

GABAA receptor agent 7 Chemical Structure

CAS No. : 2376841-18-6

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Description

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[1].

Cellular Effect
Cell Line Type Value Description References
CHO EC50
0.2 μM
Compound: 5c
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)
[PMID: 31708184]
CHO EC50
3.08 μM
Compound: 5c
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
[PMID: 31708184]
Cortical neurone IC50
0.452 μM
Compound: 5c
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
[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.

In Vivo

GABAA receptor agent 7 shows anticonvulsant activity in mice with an ED50 of 31.81 mg/kg and an TD50 of 547.89 mg/kg[1].
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.

Molecular Weight

336.78

Formula

C18H13ClN4O

CAS No.
SMILES

O=C1C=C(CC2=CC=C(Cl)C=C2)N=C3N1NC(C4=CC=CC=C4)=N3

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Purity & Documentation
References
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  • 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.

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GABAA receptor agent 7
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HY-146099
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