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6,7,8,9-四氢-5-硝基-1H-苯[g]吲哚-2,3-二酮 3-肟

用途

NS-102是一种选择性红藻氨酸(GluK2)受体拮抗剂。NS-102是一种有效的GluR6/7受体拮抗剂[1][2][3]。

名称

[ CAS 号 ]:
136623-01-3

[ 中文名 ]:
6,7,8,9-四氢-5-硝基-1H-苯[g]吲哚-2,3-二酮 3-肟

[ 英文名 ]:
NS-102

[英文别名 ]:

NS 102

生物活性

[ 描述 ]:

NS-102是一种选择性红藻氨酸(GluK2)受体拮抗剂。NS-102是一种有效的GluR6/7受体拮抗剂[1][2][3]。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

信号通路 >> 跨膜转运 >> iGluR

[体外研究]

NS-102(10μM)和GYKI 52466(30μM)的组合可防止在缺氧和葡萄糖剥夺(OGD)期间完全丧失复合动作电位(CAP)并增加CAP面积恢复[1]。

[体内研究]

NS-102(20、40或80 μmol/L；在海马CA3区)显著降低七氟醚诱导的多动症[1]。

[参考文献]

[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.

物理化学性质

[ 密度 ]:
1.74g/cm3

[ 沸点 ]:
405.8ºC at 760mmHg

[ 分子式 ]:
C₁₂H₁₁N₃O₄

[ 分子量 ]:
261.23300

[ 闪点 ]:
199.2ºC

[ 精确质量 ]:
261.07500

[ PSA ]:
107.51000

[ LogP ]:
2.13230

[ 蒸汽压 ]:
2.81E-08mmHg at 25°C

[ 折射率 ]:
1.794

[ 储存条件 ]:
2-8°C，密封，干燥

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

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...

更多文献

6,7,8,9-四氢-5-硝基-1H-苯[g]吲哚-2,3-二酮 3-肟

用途

名称

生物活性

物理化学性质

安全信息

文献

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