NS-102

Names

[ Name ]:
NS-102

[Synonym ]:
1H-Benz[g]indole-2,3-dione,6,7,8,9-tetrahydro-5-nitro-,3-oxime
NS 102
6,7,8,9-Tetrahydro-5-nitro-1H-benz[g]indole-2,3-dione 3-oxime

Biological Activity

[Description]:

NS-102 is a selective kainate (GluK2) receptors antagonist. NS-102 is a potent GluR6/7 receptor antagonist[1][2][3].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Research Areas >> Neurological Disease

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[In Vitro]

Combination of NS-102 (10 μM) and GYKI 52466 (30 μM) preventes full loss of compound action potentials (CAPs) during oxygen and glucose deprivation (OGD) and increased CAP area recovery[1].

[In Vivo]

NS-102 (20, 40 or 80 μmol/litre ; in the hippocampal CA3 region) significantly reduces Sevoflurane-induced hyperactivities[1].

[References]

[1]. Selva Baltan Tekkök, et al. Excitotoxic mechanisms of ischemic injury in myelinated white matter. J Cereb Blood Flow Metab. 2007 Sep;27(9):1540-52.

[2]. P Liang, et al. Sevoflurane activates hippocampal CA3 kainate receptors (Gluk2) to induce hyperactivity during induction and recovery in a mouse model. Br J Anaesth. 2017 Nov 1;119(5):1047-1054.

[3]. Barbara Gisabella, et al. Kainate receptor-mediated modulation of hippocampal fast spiking interneurons in a rat model of schizophrenia. PLoS One. 2012;7(3):e32483.

Chemical & Physical Properties

[ Density]:
1.74g/cm3

[ Boiling Point ]:
405.8ºC at 760mmHg

[ Molecular Formula ]:
C₁₂H₁₁N₃O₄

[ Molecular Weight ]:
261.23300

[ Flash Point ]:
199.2ºC

[ Exact Mass ]:
261.07500

[ PSA ]:
107.51000

[ LogP ]:
2.13230

[ Vapour Pressure ]:
2.81E-08mmHg at 25°C

[ Index of Refraction ]:
1.794

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

Articles

Selective block of recombinant glur6 receptors by NS-102, a novel non-NMDA receptor antagonist.

Eur. J. Pharmacol. 269 , 43, (1994)

The diversity of neuronal glutamate receptors continues to increase with the discovery of multiple subunits and subunit families. The significance of this potential receptor heterogeneity is unknown b...

A novel non-NMDA receptor antagonist shows selective displacement of low-affinity [3H]kainate binding.

Eur. J. Pharmacol. 246 , 195, (1993)

5-Nitro-6,7,8,9-tetrahydrobenzo[G]indole-2,3-dione-3-oxime (NS-102), a new competitive glutamate receptor antagonist displaced binding to non-N-methyl-D-aspartate (non-NMDA) binding sites with no acti...

Kainate receptor-mediated inhibition of presynaptic Ca2+ influx and EPSP in area CA1 of the rat hippocampus.

J. Physiol. 509 ( Pt 3) , 833-45, (1998)

1. The effect of a low concentration (1 microM) of kainate (kainic acid; KA) on presynaptic calcium (Ca2+) influx at the Schaffer collateral-commissural (SCC) synapse was examined in rat hippocampal s...