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  • (+)MK-801 maleate

    • Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801; MK801
    货号: abs810777
    CAS号: 77086-22-7
    分子式: C20H19NO4
    分子量: 337.37
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    货号-规格 货期 价格 数量
    abs810777-10mg 现货 ¥386.00
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    abs810777-100mg 1-2周 ¥2239.00
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    大包装询价
    产品描述
    描述

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

    纯度
    >98%
    储存/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.
    基本信息
    别名
    Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801; MK801
    外观
    Powder
    可溶性/溶解性
    DMSO :67 mg/mL (198.59 mM)

    Ethanol :7 mg/mL (20.74 mM)
    生物活性
    靶点
    NMDA receptor
    In vitro(体外研究)
    MK-801 labels high-affinity binding sites in rat cerebral cortical membranes in a saturable manner. MK-801 produces a potent blockade of depolarizing responses to NMDA in rat cerebral cortical slices. The only compounds that are able to compete for MK-801 binding sites are substances known to block the responses of excitatory amino acids mediated by the NMDA receptor subtype. MK-801 inhibits N-methyl-D-aspartate-induced norepinephrine (NE) release and TCP binding in the hippocampus with IC50 of 20 nM and 9 nM, respectively. MK-801 causes a progressive, long-lasting blockade of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 is also effective at blocking NMDA-activated single-channel activity in outside-out patches. MK-801 (
    In vivo(体内研究)
    Treatment of mice with MK-801 (1 mg/kg) before each METH injection reduced the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05 mg/kg or 0.2 mg/kg, i.p.) in rats just prior to reactivation of the cocaine-associated memory in the CPP context attenuates subsequent cocaine-primed reinstatement, while no disruption occurres in rats that do not receive reactivation in the CPP context. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage does not suppress subsequent cocaine-primed reinstatement.
    参考文献
    参考文献
    [1]. Wong EH, et al. Proc Natl Acad Sci U S A, 1986, 83(18), 7104-7108.
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