NBQX (FG9202)

Catalog No.S9686 Batch:S968601

Technical Data

Formula	C₁₂H₈N₄O₆S
Molecular Weight	336.28	CAS No.	118876-58-7
Solubility (25°C)*	In vitro	DMSO	67 mg/mL (199.23 mM)
		Water	Insoluble
		Ethanol	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

NBQX (FG9202, NNC 079202) is a highly selective and competitive antagonist of AMPA receptor (AMPAR) with anti-epileptic effect.

Targets

AMPAR ^[1]

In vitro

NBQX is highly selective in vitro. The IC50 value for inhibition of AMPA-evoked inward currents is 0.4 μM for NBQX. While NBQX inhibits NMDA-induced currents with IC50 value of 60 μM.^[2]

In vivo

Rats are intraperitoneally (i.p.) injected with pentylenetetrazole (PTZ, 50 mg/kg) for 28 consecutive days to establish chronic epilepsy models. Subsequently, NBQX (20 mg/kg, i.p.) is injected for 3 days for the observation of behavioral measurements of epilepsy. NBQX treatment normalizes perineuronal nets (PNNs), tenascin-R, aggrecan and neurocan levels. NBQX is sufficient to decrease seizures through increasing the latency to seizures, decrease the duration of seizure onset, and reduce the scores for the severity of seizures.^[1]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Mouse neocortical neurones Concentrations 0.1 μM - 100 μM Incubation Time -- Method Cells are continuously superfused with extracellular saline at a rate of 2.5 ml/min. After giga-seal formation the whole cell configuration is obtained by suction.The holding potential is - 60 mV and at the start of each experiment the current is measured continuously for 30 s to ensure a stable baseline. Agonist-containing solutions are delivered to the chamber through a custom-made gravity-driven flowpipe, the tip of which is placed approximately 50 μm from the cell. Application is triggered when the tubing connected to the flowpipe is compressed by a valve controlled by the Pulse software. In general, agonists are applied for 1.5 or 3 s every 45 s. The sample interval during application is 600 μs. After stable responses are obtained, the extracellular saline as well as the agonist-containing solution are replaced by solutions containing NBQX to be tested. NBQX is present until responses of a repeatable amplitude are achieved. Currents are measured at the plateau phase of the responses just before deactivation.
Animal Study:^{^[1]}	Animal Models Male Wistar rats Dosages 20 mg/kg Administration IP

Cell Assay:^{^[2]}

Cell lines
Mouse neocortical neurones
Concentrations
0.1 μM - 100 μM
Incubation Time
--
Method
Cells are continuously superfused with extracellular saline at a rate of 2.5 ml/min. After giga-seal formation the whole cell configuration is obtained by suction.The holding potential is - 60 mV and at the start of each experiment the current is measured continuously for 30 s to ensure a stable baseline. Agonist-containing solutions are delivered to the chamber through a custom-made gravity-driven flowpipe, the tip of which is placed approximately 50 μm from the cell. Application is triggered when the tubing connected to the flowpipe is compressed by a valve controlled by the Pulse software. In general, agonists are applied for 1.5 or 3 s every 45 s. The sample interval during application is 600 μs. After stable responses are obtained, the extracellular saline as well as the agonist-containing solution are replaced by solutions containing NBQX to be tested. NBQX is present until responses of a repeatable amplitude are achieved. Currents are measured at the plateau phase of the responses just before deactivation.

Animal Study:^{^[1]}

Animal Models
Male Wistar rats
Dosages
20 mg/kg
Administration
IP

References

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SHIPPING AND STORAGE
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