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1-[2-[(二苯基亚甲基)亚氨基]氧基]乙基]-1,2,5,6-四氢 3-吡啶羧酸盐酸盐

用途

NNC-711(盐酸盐)是GAT-1(GABA转运体1)的有效和选择性抑制剂,对hGAT-1的IC50为40 nM。NNC-711在体内具有抗惊厥和镇痛作用,并表现出认知增强活性[1][2][3]。

名称

[ CAS 号 ]:
145645-62-1

[ 中文名 ]:
1-[2-[(二苯基亚甲基)亚氨基]氧基]乙基]-1,2,5,6-四氢 3-吡啶羧酸盐酸盐

[ 英文名 ]:
NNC 711

[英文别名 ]:

NO-711 hydrochloride
NO 711
Nnc-711
Oxyntomodulin

生物活性

[ 描述 ]:

NNC-711(盐酸盐)是GAT-1(GABA转运体1)的有效和选择性抑制剂,对hGAT-1的IC50为40 nM。NNC-711在体内具有抗惊厥和镇痛作用,并表现出认知增强活性[1][2][3]。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> GABA受体

研究领域 >> 神经疾病

信号通路 >> 神经信号通路 >> GABA受体

[参考文献]

[1]. Borden LA, et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24.

[2]. O'Connell AW, et al. Anti-ischemic and cognition-enhancing properties of NNC-711, a gamma-aminobutyric acid reuptake inhibitor. Eur J Pharmacol. 2001 Jul 13;424(1):37-44.

[3]. Li Y,et al. Analgesic effect of intrathecally γ-aminobutyric acid transporter-1 inhibitor NO-711 administrating on neuropathic pain in rats. Neurosci Lett. 2011 Apr 20;494(1):6-9.

物理化学性质

[ 沸点 ]:
541.2ºC at 760 mmHg

[ 熔点 ]:
204 - 206 °C

[ 分子式 ]:
C₂₁H₂₃ClN₂O₃

[ 分子量 ]:
386.87200

[ 闪点 ]:
281.1ºC

[ 精确质量 ]:
386.14000

[ PSA ]:
62.13000

[ LogP ]:
3.91220

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
1.52E-12mmHg at 25°C

[ 储存条件 ]:
室温

MSDS

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

合成路线

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文献

Intracellular Na+ concentration influences short-term plasticity of glutamate transporter-mediated currents in neocortical astrocytes.

Glia 60(4) , 605-14, (2012)

Fast synaptic transmission requires a rapid clearance of the released neurotransmitter from the extracellular space. Glial glutamate transporters (excitatory amino acid transporters, EAATs) strongly c...

Attenuation of the stimulant response to ethanol is associated with enhanced ataxia for a GABA, but not a GABA, receptor agonist.

Alcohol. Clin. Exp. Res. 33(1) , 108-20, (2009)

The gamma-aminobutyric acid (GABA) system is implicated in the neurobiological actions of ethanol, and pharmacological agents that increase the activity of this system have been proposed as potential ...

GABA transporter type 1 (GAT-1) uptake inhibition reduces stimulated aspartate and glutamate release in the dorsal spinal cord in vivo via different GABAergic mechanisms.

Neuropharmacology 53(8) , 975-81, (2007)

Mechanisms through which the reported antinociceptive activity of GABA re-uptake inhibitors is mediated (and where on the sensory neuraxis) have not been defined. Here, microdialysis in the anaestheti...

更多文献

1-[2-[(二苯基亚甲基)亚氨基]氧基]乙基]-1,2,5,6-四氢 3-吡啶羧酸盐酸盐

用途

名称

生物活性

物理化学性质

MSDS

详细MSDS(安全技术说明书)

安全信息

合成路线

详细合成路线

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文献

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