NCS-382 (sodium salt)

NCS-382 (sodium salt)

CAT N°: 29315
Price:

From 140.00 119.00

NCS-382 is a ?-hydroxybutyrate receptor (GHBR) antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes, respectively, in radioligand binding assays).{46598} 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.{46599} 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.{46598}

Territorial Availability: Available through Bertin Technologies only in France

  • Synonyms
    • 2-(5,7,8,9-tetrahydro-5-hydroxy-6H-benzocyclohepten-6-ylidene)-acetic acid, monosodium salt
  • Correlated keywords
    • 520505-01-5 NCS382 antisedative
  • Product Overview:
    NCS-382 is a ?-hydroxybutyrate receptor (GHBR) antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes, respectively, in radioligand binding assays).{46598} 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.{46599} 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.{46598}

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