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(+)-MK 801 Maleate

现货
Catalog No.
A8896
NMDA拮抗剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
10mg
¥ 480.00
现货
50mg
¥ 1,860.00
现货

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Background

(+)-MK 801 is a potent antagonist of NMDA with Ki value of 30.5nM [1].

MK 801 is a potent anticonvulsant exhibits both anxiolytic and sympathomimetic properties. It is found to be a noncompetitive antagonist of NMDA. MK 801 can penetrate into the central nervous system. In the in vitro assay, MK 801 binds to rat cerebral cortical membrane with high affinity in a saturable manner. This binding is reversible even when the concentration of MK 801 is up to 100μM. It is also found that the binding shows a regional specificity. Most of these binding sites are located in the hippocampus. In rat cortical-slice preparations, MK 801 causes a potent blockade of depolarizing responses to NMDA with a high selectivity. This effect is persistent. The blockade can also cause a suppression of the epileptiform activity induced by tetrodotoxin or other neurotoxin [1].

References:
[1] Wong EH, Kemp JA, Priestley T, Knight AR, Woodruff GN, Iversen LL . The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt337.37
Cas No.77086-22-7
FormulaC20H19NO4
Solubility≥16.85mg/mL in DMSO
Chemical Name(5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate
SDFDownload SDF
Canonical SMILESC[C@]1(N2)C3=C(C=CC=C3)C[C@@H]2C4=C1C=CC=C4.O=C(O)/C=C\C(O)=O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

来自胎儿大鼠脑的原代混合神经元/胶质细胞培养物。

溶解方法

在DMSO的溶解度>16.9mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

10μM,30分钟

应用

在混合神经元/胶质细胞培养物中,NMDA诱导细胞凋亡。在轻度兴奋性毒性损伤的情况下,本研究表明MK 801对凋亡性细胞死亡的减弱作用。

动物实验 [2]:

动物模型

C57BL / 6; BALB / c小鼠

剂量

皮下或腹腔注射,0.1 mg kg(-1)

应用

对于长期性地C57BL / 6慢性应激组,MK 801防止体重增加赤字。对于C57BL / 6组,慢性MK 801产生毛皮状态的改变。在长期应激的C57BL / 6小鼠的CA1层中,MK 801诱导VGLUT1免疫反应性的增加。对于BALB / c组,MK 801增强了慢性应激组DG中的BDNF mRNA。在慢性应激的BALB / c小鼠中,MK 801阻止了CA3层中应激诱导的VGLUT3免疫反应性上调。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Wise-Faberowski L,Pearlstein RD,Warner DS., et al. NMDA-induced apoptosis in mixed neuronal/glial cortical cell cultures: the effects of isoflurane and dizocilpine. J Neurosurg Anesthesiol.2006 Oct;18(4):240-6.

[2].Farley S, Dumas S, El Mestikawy S ., et al. Increased expression of the Vesicular Glutamate Transporter-1 (VGLUT1) in the prefrontal cortex correlates with differential vulnerability to chronic stress in various mouse strains: effects of fluoxetine and MK-801. Neuropharmacology. 2012 Jan;62(1):503-17.

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