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(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸

(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸用途

CGP 37849 是一种有效的竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。CGP 37849 是啮齿动物的抗惊厥药,具有抗抑郁和抗焦虑作用。

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(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸名称

[ CAS 号 ]:
127910-31-0

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

[ 英文名 ]:
CGP 37849

[英文别名 ]:

Proglumide sodium salt
E-2-amino-4-methyl-5-phosphono-3-pentenoic acid
dl-2-amino-4-methyl-5-phosphono-3-*pentenoic acid

(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸生物活性

[ 描述 ]:

CGP 37849 是一种有效的竞争性口服活性 N-甲基-D-天冬氨酸 (NMDA) 受体拮抗剂。CGP 37849 是啮齿动物的抗惊厥药,具有抗抑郁和抗焦虑作用。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> iGluR

信号通路 >> 跨膜转运 >> iGluR

[体外研究]

在体外海马切片中,CGP 37849选择性地和可逆地拮抗NMDA诱发的CA1锥体细胞放电率的增加。在沐浴在含有低Mg2+水平的培养基中的切片中,CGP 37,849浓度高达10μM通过刺激Schaffer侧支连合纤维抑制CA1神经元中诱发的爆发放电,而不影响初始群体峰值的大小[1]。

[体内研究]

CGP 37849有效(Ki为220 nM)并竞争性抑制NMDA敏感的l-[3H]-谷氨酸与大鼠脑突触后密度(PSD)fractin的结合。CGP 37849抑制选择性NMDA受体拮抗剂,[3H]-(±)-3-(2-羧基哌嗪-4-基)丙基-1-膦酸酯(CPP)的结合,Ki为35 nM[1]。。在体内,对CGP 37,849大鼠的口服给药选择性地阻断由离子电泳应用的NMDA诱导的海马神经元中的放电,而不影响对quisqualate或红藻氨酸盐的反应[1]。对CGP 37,849小鼠的口服给药抑制ED50为21mg/kg的小鼠中最大电休克诱导的癫痫发作[1]。

[参考文献]

[1]. Fagg GE, 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.

[2]. Schmutz M, et al. The competitive NMDA receptor antagonists CGP 37849 and CGP 39551 are potent, orally-active anticonvulsants in rodents. Naunyn Schmiedebergs Arch Pharmacol. 1990 Jul;342(1):61-6.

[3]. Papp M, et al. Antidepressant activity of non-competitive and competitive NMDA receptor antagonists in a chronic mild stress model of depression. Eur J Pharmacol. 1994 Sep 22;263(1-2):1-7.

[4]. Przegaliński E, et al. The influence of the benzodiazepine receptor antagonist flumazenil on the anxiolytic-like effects of CGP 37849 and ACPC in rats. Neuropharmacology. 2000 Jul 24;39(10):1858-64.

(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸物理化学性质

[ 密度 ]:
1.506 g/cm3

[ 沸点 ]:
523.1ºC at 760 mmHg

[ 分子式 ]:
C₆H₁₂NO₅P

[ 分子量 ]:
209.13700

[ 闪点 ]:
270.2ºC

[ 精确质量 ]:
209.04500

[ PSA ]:
130.66000

[ LogP ]:
0.22260

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
2-8℃，干燥，密闭

(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸MSDS

详细MSDS(安全技术说明书)

(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

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

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(E)-2-氨基-4-甲基-5-膦酰基-3-戊烯酸文献

Involvement of voltage- and ligand-gated Ca2+ channels in the neuroexcitatory and synergistic effects of putative uremic neurotoxins.

Kidney Int. 63(5) , 1764-75, (2003)

Renal failure has been viewed as a state of cellular calcium toxicity due to the retention of small fast-acting molecules. We have tested this hypothesis and identified potentially neuroexcitatory com...

GSA: behavioral, histological, electrophysiological and neurochemical effects.

Physiol. Behav. 84(2) , 251-64, (2005)

Renal insufficient patients suffer from a variety of complications as direct and indirect consequence of accumulation of retention solutes. Guanidinosuccinic acid (GSA) is an important probable uremic...

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...

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