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NCS-382 (sodium salt) Sale

目录号 : GC45991

A GHB receptor antagonist

NCS-382 (sodium salt) Chemical Structure

Cas No.:131733-92-1

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10mg
¥1,284.00
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50mg
¥5,791.00
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100mg
¥10,278.00
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Sample solution is provided at 25 µL, 10mM.

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

|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).

化学性质

Cas No. 131733-92-1 SDF
Canonical SMILES OC(C1=CC=CC=C1CCC/2)C2=C\C([O-])=O.[Na+]
分子式 C13H13O3.Na 分子量 240.2
溶解度 DMF: 20 mg/ml,DMSO: 12 mg/ml,Ethanol: 5 mg/ml,PBS (pH 7.2): 10 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 4.1632 mL 20.816 mL 41.632 mL
5 mM 0.8326 mL 4.1632 mL 8.3264 mL
10 mM 0.4163 mL 2.0816 mL 4.1632 mL
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