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NCS-382 (sodium salt)

Katalog-Nr.GC45991

A GHB receptor antagonist

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NCS-382 (sodium salt) Chemische Struktur

Cas No.: 131733-92-1

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10mg
128,00 $
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50mg
579,00 $
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100mg
1.028,00 $
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Sample solution is provided at 25 µL, 10mM.

Description Chemical Properties Product Documents Related Products

NCS-382 is a γ-hydroxybutyrate receptor (GHBR) antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes, respectively, in radioligand binding assays).1 It is selective for GHBR over GABA binding sites in rat brain synaptic membranes at concentrations of 1 and 10 μM. NCS-382 decreases GHB-induced increases in inositol phosphate accumulation and cGMP levels in isolated rat hippocampal slices (IC50s = 8.6 and 30 μM, respectively). It reduces GHB-induced increases in the time mice spent immobile in the forced swim test, indicating anti-sedative activity, when administered at doses of 1.66 and 2.08 mmol/kg.2 NCS-382 decreases spike and wave discharges in audiogenic seizure-susceptible Swiss Rb mice, as well as a rat model of petit mal epilepsy, when administered at a dose of 2.3 mmol/kg.1

|1. Maitre, M., Hechler, V., Vayer, P., et al. A specific γ-hydroxybutyrate receptor ligand possesses both antagonistic and anticonvulsant properties. J. Pharmacol. Exp. Ther. 255(2), 657-663 (1990).|2. Schmidt, C., Gobaille, S., Hechler, V., et al. Anti-sedative and anti-cataleptic properties of NCS-382, a γ-hydroxybutyrate receptor antagonist. Eur. J. Pharmacol. 203(3), 393-397 (1991).

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