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NCS-382(sodium salt)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NCS-382(sodium salt)图片
CAS NO:131733-92-1
包装与价格:
包装价格(元)
10mg电议
50mg电议
100mg电议

产品介绍
A GHB receptor antagonist
Cas No.131733-92-1
Canonical SMILESOC(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
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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).