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NCS-382 sodium

Cat. No. M42191
NCS-382 sodium Structure
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Biological Activity

NCS-382 (sodium) is a potent GABA receptor antagonist.

Chemical Information
Molecular Weight 240.23
Formula C13H13NaO3
CAS Number 131733-92-1
Form Solid
Storage Powder -20°C 3 years
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] P S van Nieuwenhuijzen et al. Neuroscience. Regional Fos-expression induced by γ-hydroxybutyrate (GHB): comparison with γ-butyrolactone (GBL) and effects of co-administration of the GABAB antagonist SCH 50911 and putative GHB antagonist NCS-382

[2] Tina Bay et al. Biochem Pharmacol. GHB receptor targets in the CNS: focus on high-affinity binding sites

[3] Maharaj K Ticku et al. Ann N Y Acad Sci. Characterization and pharmacology of the GHB receptor

[4] C Schmidt et al. Eur J Pharmacol. Anti-sedative and anti-cataleptic properties of NCS-382, a gamma-hydroxybutyrate receptor antagonist

[5] G Tunnicliff. Gen Pharmacol. Significance of gamma-hydroxybutyric acid in the brain

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