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L-701324

货号:A560344

L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor.

L-701324 化学结构 CAS号:142326-59-8
L-701324 化学结构
CAS号:142326-59-8
L-701324 3D分子结构
CAS号:142326-59-8
L-701324 化学结构 CAS号:142326-59-8
L-701324 3D分子结构 CAS号:142326-59-8
规格 价格 库存 数量
10mM*1mL(DMSO) ¥630 咨询
5mg ¥381 咨询
10mg ¥623 咨询
25mg ¥1088 咨询
50mg ¥1843 咨询
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L-701324 纯度/质量文件 产品仅供科研

货号:A560344 标准纯度:
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产品名称 NMDA receptor 其他靶点 纯度
Empirical Formula 97%
Dizocilpine maleate +++

NMDA receptor, Kd: 37.2 nM

99%+
Felbamate +

NMDAR, IC50: 1.8 mM

98%
(-)-Dizocilpine maleate ++++

NMDA receptor, Ki: 30.5 nM

98%
Ifenprodil tartrate +++

NMDA Receptor, IC50: 0.3 μM

98%
Spermidine Autophagy 98% GC
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

L-701324 生物活性

描述 L-701324 is an orally active and long acting anticonvulsant with high affinity and selectivity for the glycine site on the NMDA receptor. L-701,324 produced a marked increase in the seizure threshold, which was significantly reversed by the administration of glycine[3]. In contrast to N-methyl-D-aspartate receptor ion channel blockers such as MK-801 (dizocilpine), L-701,324 is a potent, p.o. active anticonvulsant with a reduced propensity to activate mesolimbic dopaminergic systems in rodents[4]. L-701324 (2.5-40 mg/kg, i.p.) dose-dependently decreased the muscle tone enhanced by haloperidol (1-5 mg/kg, i.p.). L-701324 exhibits a beneficial action in the animal model of parkinsonian rigidity, but not that of parkinsonian akinesia[5]. Pretreatment with L-701,324 dose-dependently antagonized amphetamine-induced hyperactivity in the mouse (ED50 = 1.12 +/- 0.45 mg/kg p.o.), an effect which was similar to that of the classical neuroleptic, haloperidol, and the atypical neuroleptic, clozapine. In addition, p.o. administration of L-701,324 (2.5 or 5 mg/kg) attenuated the hyperactivity response induced by amphetamine infusion into the rat nucleus accumbens. L-701,324 failed to impair spontaneous locomotor activity or induce catalepsy in the mouse at doses > or = 100 mg/kg[6]. Moreover, anticonvulsant and neuroprotective actions of L-701,324 may not be associated with marked anaesthesia-like side-effects[7].

L-701324 参考文献

[1]Bristow LJ, Flatman KL, et al. The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents. J Pharmacol Exp Ther. 1996 May;277(2):578-85.

[2]Bristow LJ, Hutson PH, et al. Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther. 1996 Nov;279(2):492-501.

[3]Wlaź P, Poleszak E. Differential effects of glycine on the anticonvulsant activity of D-cycloserine and L-701,324 in mice. Pharmacol Rep. 2011;63(5):1231-4

[4]Bristow LJ, Hutson PH, Kulagowski JJ, Leeson PD, Matheson S, Murray F, Rathbone D, Saywell KL, Thorn L, Watt AP, Tricklebank MD. Anticonvulsant and behavioral profile of L-701,324, a potent, orally active antagonist at the glycine modulatory site on the N-methyl-D-aspartate receptor complex. J Pharmacol Exp Ther. 1996 Nov;279(2):492-501

[5]Konieczny J, Ossowska K, Schulze G, Coper H, Wolfarth S. L-701,324, a selective antagonist at the glycine site of the NMDA receptor, counteracts haloperidol-induced muscle rigidity in rats. Psychopharmacology (Berl). 1999 Apr;143(3):235-43

[6]Bristow LJ, Flatman KL, Hutson PH, Kulagowski JJ, Leeson PD, Young L, Tricklebank MD. The atypical neuroleptic profile of the glycine/N-methyl-D-aspartate receptor antagonist, L-701,324, in rodents. J Pharmacol Exp Ther. 1996 May;277(2):578-85

[7]Obrenovitch TP, Hardy AM, Zilkha E. Effects of L-701,324, a high-affinity antagonist at the N-methyl-D-aspartate (NMDA) receptor glycine site, on the rat electroencephalogram. Naunyn Schmiedebergs Arch Pharmacol. 1997 Jun;355(6):779-86

L-701324 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.75mL

0.55mL

0.27mL

13.74mL

2.75mL

1.37mL

27.49mL

5.50mL

2.75mL

L-701324 技术信息

CAS号142326-59-8
分子式C21H14ClNO3
分子量 363.794
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,Room Temperature

溶解度

DMSO: 35 mg/mL(96.21 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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