GABAA receptor modulator-9
GABAA receptor modulator-9 is and positive allosteric modulator of a1β2y2 subtype GABAA 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).
For research use only. We do not sell to patients.
- Formula: C23H17N3OS2
- Molecular Weight:415.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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 GABAARs[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Pilocarpine-induced status epilepticus (SE) models established in male C57BL/6N mice (6−8 weeks old, 18-20 g)[1]
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Dosage:5, 10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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Result:Exhibited potent therapeutic efficacy, preventing 90% of Stage V seizure onset at 30 mg/kg.
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Animal Model:Pentylenetetrazole (PTZ)-induced acute convulsive seizures model established in male C57BL/6N mice (6−8 weeks old, 18-20 g)[1]
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Dosage:5, 10 and 30 mg/kg
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Administration:Intraperitoneal injection (i.p.), single dose
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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.
Chemical Information
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Molecular Weight 415.53
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Formula C23H17N3OS2
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SMILES
O=C1N(C(c2ccccc2)=NC3=C1SC(C4=CC=CS4)=N3)C5=CC=CC=C5CC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GABAA receptor modulator-9 Related Classifications
HY-175251 Related Classifications
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