GABAA receptor modulator-8

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GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity.

For research use only. We do not sell to patients.

GABAA receptor modulator-8 Chemical Structure

CAS No. : 2889382-34-5

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Purity & Documentation
References
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Description

GABAA receptor modulator-8 (10c) is a blood-brain barrier penetrated, selective and positive modulator of GABAA receptor, with excellent antiepileptic activity^[1].

Parmacokinetics^[1]

Species	Dose	Route	Indicator	value
Rat	10 mg/kg	i.g.	T_max	4 hr
Rat	10 mg/kg	i.v.	T_1/2	2.47±0.14 hr
Rat	30 mg/kg	i.g.	T_max	4 hr
Rat	30 mg/kg	i.v.	T_1/2	2.49±0.07 hr
Rat	10 mg/kg	i.g.	C_max	587.67±12.66 ng/mL
Rat	10 mg/kg	i.v.	MRT_0-t	3.65±0.30 hr
Rat	30 mg/kg	i.g.	C_max	1521.25±100.76 ng/mL
Rat	30 mg/kg	i.v.	MRT_0-t	3.86±0.06 hr
Rat	10 mg/kg	i.g.	T_1/2	2.53±0.12 hr
Rat	10 mg/kg	i.v.	AUC_0-t	34,263.98±1100.87 ng/L.h
Rat	30 mg/kg	i.g.	T_1/2	2.57±0.09 hr
Rat	30 mg/kg	i.v.	AUC_0-t	107,689.72±6779.70 ng/L.h
Rat	10 mg/kg	i.g.	MRT_0-t	4.57±0.09 hr
Rat	10 mg/kg	i.v.	AUC_0-∞	34,341.50±908.33 ng/L.h
Rat	30 mg/kg	i.g.	MRT_0-t	5.37±0.32 hr
Rat	30 mg/kg	i.v.	AUC_0-∞	108,414.07±5853.89 ng/L.h
Rat	10 mg/kg	i.g.	AUC_0-t	3201.38±82.07 ng/L.h
Rat	30 mg/kg	i.g.	AUC_0-t	11,273.22±703.84 ng/L.h
Rat	10 mg/kg	i.g.	AUC_0-∞	3202.48±80.91 ng/L.h
Rat	30 mg/kg	i.g.	AUC_0-∞	11,328.84±574.48 ng/L.h
Rat	10 mg/kg	i.g.	F	9.34±0.07 %
Rat	30 mg/kg	i.g.	F	10.47±0.10 %

In Vivo

GABAA receptor modulator-8 (10c) exhibits excellent antiepileptic activity with ED₅₀ value of 8.51 mg/kg in the maximal electroshock (MES) model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

348.37

Formula

C₂₀H₁₇FN₄O

CAS No.

2889382-34-5

SMILES

CCCOC1=CC(C2=CC=CC=C2)=NC3=NC(C4=C(F)C=CC=C4)=NN13

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]. Han Liang, et al. Pharmacokinetics and Tissue Distribution Study for 2-(2-Fluorophenyl)-5-Phenyl-7-Alkoxy- [1,2,4]Triazole[1,5-a]Pyrimidine Antiepileptic Compounds in Rats. Biomed Chromatogr. 2025 May;39(5):e70088. [Content Brief]