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Ganaxolone (CCD 1042), an orally active synthetic analog of the neuroactive steroid allopregnanolone, is a selective, high-affinity positive allosteric modulator of gamma-aminobutyric acid-A (GABA_A) receptor with anticonvulsant properties. Ganaxolone acts through binding sites which are distinct from the benzodiazepine binding site.

Ganaxolone inhibits binding of the γ-aminobutyric acid (GABA_A) receptor-chloride channel ligand t-[S]butylbicyclophosphorothionate (IC₅₀ of 80 nM) and enhanced binding of the benzodiazepine site ligand [H]flunitrazepam (EC₅₀ of 125 nM) and the GABA site ligand [H]muscimol (EC₅₀ of 86 nM).

Ganaxolone (3.75-30 mg/kg, s.c.) injected 60 min before testing of socially isolated (SI) mice, induces a dose-dependent reduction in aggression toward a same-sex intruder and anxiety-like behavior in an elevated plus maze ( EC₅₀=10 mg/kg).
Ganaxolone (5-30 mg/kg; IP; 10 minutes prior to administration of either pentyle-netetrazol orγ-butyrolactone; drug-naive male Sprague Dawley rats) exacerbates seizures in animal models of absence.

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