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抑制剂描述:

产品名称:MK-801 (Dizocilpine)

产品别名:见爱必信官网

英文别名:MK-801 (Dizocilpine)

靶点:NMDAR

CAS:77086-21-6

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.

溶解性:Ethanol :7mg/mL(31.63mM)
DMSO :67 mg/mL (302.75 mM)

体外研究:

Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches.
Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.

体内研究:Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.

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