GABAA receptor agent 8

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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.

GABAA receptor agent 8 Chemical Structure

CAS No. : 2376841-54-0

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

GABAA receptor^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.24 μM Compound: 5e	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	12.02 μM Compound: 5e	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	0.334 μM Compound: 5e	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 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.

In Vivo

GABAA receptor agent 8 (compoud 5e) shows anticonvulsant activity in mice with an ED₅₀ of 40.95 mg/kg and an TD₅₀ of 372.39 mg/kg^[1].
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.

Molecular Weight

316.36

Formula

C₁₉H₁₆N₄O

CAS No.

2376841-54-0

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Huang L, et al. Discovery of [1,2,4]-triazolo [1,5-a]pyrimidine-7(4H)-one derivatives as positive modulators of GABAA1 receptor with potent anticonvulsant activity and low toxicity. Eur J Med Chem. 2020 Jan 1;185:111824. [Content Brief]