A GHBR antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes

NCS-382 (sodium salt) – 50 mg

Brand:
Cayman
CAS:
131733-92-1
Storage:
-20
UN-No:
Non-Hazardous - /

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).{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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SKU: 29315 - 50 mg Category:

Description

A GHBR antagonist (IC50s = 134.1 and 201.3 nM in isolated rat striatal and hippocampal membranes, respectively, in radioligand binding assays); selective for GHBR over GABA binding sites in rat brain synaptic membranes at 1 and 10 µM; decreases GHB-induced increases in inositol phosphate accumulation and cGMP levels in isolated rat hippocampal slices (IC50s = 8.6 and 30 µM, respectively); reduces GHB-induced increases in the time mice spent immobile in the forced swim test at 1.66 and 2.08 mmol/kg; decreases spike and wave discharges in audiogenic seizure-susceptible Swiss Rb mice, as well as a rat model of petit mal epilepsy, at 2.3 mmol/kg

Formal name: 2-(5,7,8,9-tetrahydro-5-hydroxy-6H-benzocyclohepten-6-ylidene)-acetic acid, monosodium salt

Synonyms: 

Molecular weight: 240.2

CAS: 131733-92-1

Purity: ≥95%

Formulation: A crystalline solid

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