A GHB receptor antagonist
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NCS-382 (sodium salt)

Item No. 29315

Technical Information
Formal Name
2-(5,7,8,9-tetrahydro-5-hydroxy-6H-benzocyclohepten-6-ylidene)-acetic acid, monosodium salt
CAS Number
131733-92-1
Molecular Formula
C13H13O3 • Na
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 20 mg/mlDMSO: 12 mg/mlEthanol: 5 mg/mlPBS (pH 7.2): 10 mg/ml
SMILES
OC(C1=CC=CC=C1CCC/2)C2=C\C([O-])=O.[Na+]
InChi Code
InChI=1S/C13H14O3.Na/c14-12(15)8-10-6-3-5-9-4-1-2-7-11(9)13(10)16;/h1-2,4,7-8,13,16H,3,5-6H2,(H,14,15);/q;+1/p-1/b10-8+;
InChi Key
BTWDZCORIHHOPO-VRTOBVRTSA-M
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Maitre, M., Hechler, V., Vayer, P., et alA 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 alAnti-sedative and anti-cataleptic properties of NCS-382, a γ-hydroxybutyrate receptor antagonist. Eur. J. Pharmacol. 203(3), 393-397 (1991).