GABAA receptor modulator-9

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GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABA_A that can cross the blood-brain barrier. GABAA receptor modulator-9 exhibits comparable activity on α1β2γ2 (EC₅₀: 0.9 μM in oocytes, 0.2 μM in CHO cells) and on α1β2, α3β2γ2 and α1β3γ2 (EC₅₀s of 1.3, 3.4 and 1.1 μM). GABAA receptor modulator-9 significantly suppresses seizure progression and reduces delayed mortality. GABAA receptor modulator-9 can be used for the study of status epilepticus (SE).

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GABAA receptor modulator-9 Chemical Structure

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Biological Activity
Purity & Documentation
References
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Description

In Vitro

GABAA receptor modulator-9 (Compound (S)-9d) demonstrates the highest selectivity for the α1 subunit, may not exhibit β subunit selectivity and the γ2 subunit does not influence its allosteric activity on GABA_ARs^[1].

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

In Vivo

GABAA receptor modulator-9 (Compound (S)-9d) (5-30 mg/kg, i.p., single dose) prevents stage V seizures in 90% of mice and significantly delays the onset of clonic seizures in Pilocarpine (HY-B0726A)-induced SE model and Pentylenetetrazole-induced acute convulsive seizure model^[1].

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

Animal Model:	Pilocarpine-induced status epilepticus (SE) models established in male C57BL/6N mice (6−8 weeks old, 18-20 g)^[1]
Dosage:	5, 10 and 30 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose
Result:	Exhibited potent therapeutic efficacy, preventing 90% of Stage V seizure onset at 30 mg/kg.

Animal Model:	Pentylenetetrazole (PTZ)-induced acute convulsive seizures model established in male C57BL/6N mice (6−8 weeks old, 18-20 g)^[1]
Dosage:	5, 10 and 30 mg/kg
Administration:	Intraperitoneal injection (i.p.), single dose
Result:	Showed reduced seizure suppression compared to diazepam at equivalent doses during the acute 2 h SE phase at 5 mg/kg. Achieved 90% prevention of Stage V seizures and significantly delayed the latency to Stage III seizure onset at 30 mg/kg. Induced mild sedative side effects at doses above 20 mg/kg.

Molecular Weight

415.53

Formula

C₂₃H₁₇N₃OS₂

SMILES

O=C1N(C(c2ccccc2)=NC3=C1SC(C4=CC=CS4)=N3)C5=CC=CC=C5CC

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]. Liao W, et al. Novel 2-(2-Thienyl)-thiazolo[4,5-d]pyrimidin-7(6H)-ones Binding β+/α- Subunit Interface as GABAAR Positive Allosteric Modulator for the Treatment of Status Epilepticus in Mouse. J Med Chem. 2025 Jul 10. [Content Brief]