|(5S,10R)-5-甲基-10,11-二氢-5H-5,10-环氨基二苯并[a,d][7]轮烯马来酸盐|CsnPharm

CAS No.: 77086-22-7

Dizocilpine maleate/地卓亚平马来酸盐 Catalog No. CSN13883

Synonyms: MK-801 maleate;Dizocilpine Maleate;Dizocilpine Hydrogen Maleate

(+)-MK 801 Maleate is a highly potent, selective and non-competitive NMDA receptor antagonist with Ki of 30.5 nM.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 NMDAR

Ki:30.5nM
描述N-Methyl-D-aspartic acid receptors (NMDAR) are a family of neurotransmitter receptors that mediate the action of excitatory amino acids in signal transduction. (+)-MK-801 maleate is a potent, selective, and non-competitive NMDAR antagonist with K_d values of 37.6, 37.2, 40.0 and 56.2 nM in rat brain membranes from hippocampus, cortex, striatum and medulla-pons, respectively^[1]. In rat hippocampal tissue, MK-801 inhibited [³H]TCP binding, NMDA-induced [³H]norepinephrine (NE) release, and [³H]NE uptake with IC50 values of 9, 20, and 2030 nM, respectively^[2]. In cultured cortical neurons, 10 μM MK-801 blocked NMDA-stimulated current with a time constant of around 11 seconds. MK-801 at 2 μM blocked NMDA-induced unitary currents in outside-out patches^[3]. The activation of microglia induced by LPS (100 mg/mL) was inhibited by 50 – 500 μM MK-801 at a dose-dependent manner. MK-801 from 50 – 500 μM also decreased Tat₇₂-stimulated (200 ng/mL) increase in Cox-2 protein expression in BV-2 cells. In mice received i.p. administration of METH, pre-treatment of MK-801 (1 mg/kg) 15 min prior to METH injection resulted in 55% reduction of DA depletion. The effect of METH on microglia activation in the striatum of mice was also significantly attenuated by the same treatment of MK-801^[4].
作用机制(+)-MK-801 maleate inhibits NMDAR by abolishing depolarizing responses to NMDA^[1].

动物研究
剂量	Mice: 0.5 mg/kg^[5] (p.o. or i.p.) Rat: 0.05 mg/kg - 0.2 mg/kg^[6] (i.p.), 0.3 mg/kg - 0.8 mg/kg^[7] (i.p.); 0.5 mg/kg - 5 mg/kg^[8] (s.c.); 10 mg/kg^[8] (i.p.)
给药途径	p.o., i.p., s.c.

参考文献

[1] Thomas DM, Kuhn DM. MK-801 and dextromethorphan block microglial activation and protect against methamphetamine-induced neurotoxicity. Brain Res. 2005;1050(1-2):190-8
[2] Snell LD, Yi SJ, et al. Comparison of the effects of MK-801 and phencyclidine on catecholamine uptake and NMDA-induced norepinephrine release. Eur J Pharmacol. 1988;145(2):223-6.
[3] Huettner JE, Bean BP. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. Proc Natl Acad Sci U S A. 1988;85(4):1307-11.
[4] Thomas DM, Kuhn DM. MK-801 and dextromethorphan block microglial activation and protect against methamphetamine-induced neurotoxicity. Brain Res. 2005;1050(1-2):190-8.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9641 mL
- 14.8205 mL
- 29.6410 mL
- 5 mM
- 0.5928 mL
- 2.9641 mL
- 5.9282 mL
- 10 mM
- 0.2964 mL
- 1.4821 mL
- 2.9641 mL

技术信息

CAS号

77086-22-7

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H19NO4

运输

蓝冰

分子量

337.37

别名

MK-801 maleate;Dizocilpine Maleate;Dizocilpine Hydrogen Maleate;(+)-MK-801 (hydrogen maleate);Dizocilpine;MK-801;地卓亚平马来酸盐

溶解度

DMSO	500.0 mg/mL (1482.1 mM) warming
Water	12.0 mg/mL (35.6 mM) warming

动物实验配方

0.5% CMC-Na

50 mg/mL

suspension

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Dizocilpine maleate/地卓亚平马来酸盐 Catalog No. CSN13883

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