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(E)-4-(乙氧羰基)-4-氨基-2-甲基丁-2-烯基膦酸

用途

CGP 39551是一种有效的口服活性竞争性N-甲基-D-天冬氨酸(NMDA)受体拮抗剂,具有有效的抗惊厥活性[1]。CGP 39551在L-[3H]-谷氨酸(Ki=8.4μM)[2]上显示出可测量的抑制活性。

名称

[ CAS 号 ]:
127910-32-1

[ 中文名 ]:
(E)-(+/-)-2-氨基-4-甲基-5-磷-3-戊烯酸乙酯

[ 英文名 ]:
CGP 39551

[英文别名 ]:

生物活性

[ 描述 ]:

[ 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]

CGP 39551抑制选择性NMDA受体拮抗剂[3H]-CPP与Ki为310 nM的大鼠脑突触后密度(PSD)的结合[2]。

[体内研究]

CGP 39551在ED50为4 mg/kg(p.o.)的小鼠中表现出最大的电击诱发癫痫发作[2]。使用CGP 39551对新生儿进行慢性治疗后,成年大鼠对D2多巴胺受体刺激的行为反应增强[3]。

[参考文献]

[1]. G E Fagg,et al. CGP 37849 and CGP 39551: novel competitive N-methyl-D-aspartate receptor antagonists with potent oral anticonvulsant activity. Prog Clin Biol Res. 1990;361:421-7.

[2]. G E Fagg, et al. CGP 37849 and CGP 39551: novel and potent competitive N-methyl-D-aspartate receptor antagonists with oral activity. Br J Pharmacol. 1990 Apr;99(4):791-7.

[3]. R Dall'Olio, et al. Chronic neonatal blockade of N-methyl-D-aspartate receptor by CGP 39551 increases dopaminergic function in adult rat. Neuroscience. 1994 Nov;63(2):451-5.

物理化学性质

[ 密度 ]:
1.312 g/cm3

[ 沸点 ]:
434.1ºC at 760 mmHg

[ 熔点 ]:
236-239ºC

[ 分子式 ]:
C₈H₁₆NO₅P

[ 分子量 ]:
237.19

[ 闪点 ]:
216.3ºC

[ 精确质量 ]:
237.07700

[ PSA ]:
119.66000

[ LogP ]:
0.70110

[ 外观性状 ]:
白色固体

[ 蒸汽压 ]:
9.46E-09mmHg at 25°C

[ 折射率 ]:
1.512

[ 储存条件 ]:
-20°C，密封，干燥

MSDS

详细MSDS(安全技术说明书)

安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

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文献

Competitive NMDA receptor antagonists and agonists: effects on spontaneous alternation in mice exposed to cerebral oligemia.

Pol. J. Pharmacol. 56(1) , 59-66, (2004)

The purpose of the present study was to investigate the effects of competitive NMDA receptor antagonists,D,L-(E)-2-amino-4-methyl-5-phosphono-3-pentenoic acid (CGP 37849) and its ethyl ester (CGP 3955...

NMDA receptor antagonists acting at the glycineB site in rat models for antipsychotic-like activity.

J. Neural Transm. Gen. Sect. 106(11-12) , 1189-204, (1999)

Several partial agonist and full antagonists acting at the glycine site of the NMDA receptors were tested for potential antipsychotic-like properties in rats. As models, amphetamine- and phencyclidine...

Effects of competitive NMDA receptor antagonists on excitatory amino acid-evoked currents in mouse spinal cord neurones.

Fundam. Clin. Pharmacol. 13(1) , 67-74, (1999)

The effects of CGP 37849 [DL-(E)-2-amino-4-methyl-5-phosphono-3-pentenoate] and its ethylester CGP 39551 on whole-cell currents evoked by the endogenous excitatory amino acids, L-glutamate and L-aspar...

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