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依利罗地

依利罗地用途

Eliprodil(SL-820715)是NR2B-NMDA受体高效选择性抑制剂,IC50值1uM,对NR2A-和NR2C-NMDA受体作用弱。

依利罗地名称

[ CAS 号 ]:
119431-25-3

[ 中文名 ]:
依利罗地

[ 英文名 ]:
Eliprodil

[英文别名 ]:

eliprodil

依利罗地生物活性

[ 描述 ]:

Eliprodil(SL-820715)是NR2B-NMDA受体高效选择性抑制剂,IC50值1uM,对NR2A-和NR2C-NMDA受体作用弱。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> iGluR

信号通路 >> 神经信号通路 >> iGluR

研究领域 >> 神经疾病

[参考文献]

[1]. Bath CP, et al. The effects of ifenprodil and eliprodil on voltage-dependent Ca2+ channels and in gerbil global cerebral ischaemia. Eur J Pharmacol. 1996 Mar 28;299(1-3):103-12.

[2]. Lengyel C, et al. Effect of a neuroprotective drug, eliprodil on cardiac repolarisation: importance of the decreased repolarisation reserve in the development of proarrhythmic risk. Br J Pharmacol. 2004 Sep;143(1):152-8.

[相关活性小分子]

依利罗地物理化学性质

[ 密度 ]:
1.205 g/cm3

[ 沸点 ]:
474.1ºC at 760 mmHg

[ 分子式 ]:
C₂₀H₂₃ClFNO

[ 分子量 ]:
347.85400

[ 闪点 ]:
240.5ºC

[ 精确质量 ]:
347.14500

[ PSA ]:
23.47000

[ LogP ]:
4.40510

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
8.57E-10mmHg at 25°C

[ 折射率 ]:
1.58

[ 储存条件 ]:
2-8°C

依利罗地安全信息

[ 符号 ]:

GHS07, GHS09

[ 信号词 ]:
Warning

[ 危害声明 ]:
H319-H410

[ 警示性声明 ]:
P273-P305 + P351 + P338-P501

[ 个人防护装备 ]:
Eyeshields;Gloves

[ 危害码 (欧洲) ]:
N: Dangerous for the environment;

[ 风险声明 (欧洲) ]:
R50/53

[ 安全声明 (欧洲) ]:
60-61

[ 危险品运输编码 ]:
UN 3077 9/PG 3

[ 海关编码 ]:
2933399090

依利罗地海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

依利罗地文献

NMDA receptor antagonists do not block the development of sensitization of catalepsy, but make its expression state-dependent.

Behav. Pharmacol. 12(2) , 143-9, (2001)

Dopamine (DA) receptor blockade induces catalepsy in rats which increases in strength upon retesting. This increase in catalepsy represents a form of sensitization which has been shown to be completel...

Synthesis and resolution of racemic eliprodil and evaluation of the enantiomers of eliprodil as NMDA receptor antagonists.

Bioorg. Med. Chem. Lett. 10(12) , 1377-80, (2000)

A short synthesis of the NMDA receptor antagonist (rac)-Eliprodil (9) and its resolution into the enantiomers by chiral HPLC is described. The enantiomers (R)-9 and (S)-9 were found to exhibit markedl...

The sequential analysis of repeated binary responses: a score test for the case of three time points.

Stat. Med. 25(13) , 2196-214, (2006)

In this paper a robust method is developed for the analysis of data consisting of repeated binary observations taken at up to three fixed time points on each subject. The primary objective is to compa...

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