Dizocilpine maleate

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Chemical Structure| 77086-22-7 同义名 : 地佐环平马来酸盐;(+)-MK 801 顺丁烯二酸盐 ;MK-801 maleate; (+)-MK-801(hydrogen maleate); Dizocilpine; (+)-Dizocilpine Maleate; (+)-MK 801 Maleate
CAS号 : 77086-22-7
货号 : A194394
分子式 : C20H19NO4
纯度 : 99%+
分子量 : 337.37
MDL号 : MFCD00082465
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：

PO 0.5% CMC-Na 50 mg/mL suspension

生物活性
靶点

  • NMDA receptor

    NMDA receptor, Kd:37.2 nM

  • NMDA receptor

    NMDA receptor, Kd:37.2 nM
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 Kd 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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL
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.