基本属性 生物活性体外研究体内研究 MSDS 用途与合成方法 供应商 相关产品
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(-)-MK801MALEATE

基本属性 生物活性体外研究体内研究 MSDS 用途与合成方法 供应商 相关产品
(-)-MK801MALEATE
(-)-MK801MALEATE 性质
  • 溶解度 DMSO: >20 mg/mL
  • 形态solid
  • 颜色white
(-)-MK801MALEATE 用途与合成方法
  • 生物活性(-)-MK 801 Maleate作用于大鼠脑组织膜,是一种有效的,选择性的,非竞争性NMDA受体拮抗剂,Kd为37.2 nM。
  • 体外研究[3H]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 [3H]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 [3H]norepinephrine (NE) release and [3H]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 (< 500 μM) prevents LPS-induced activation of microglia in a concentration-dependent manner with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with EC50 of 400 μM in BV-2 cells.
  • 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.
安全信息
  • 安全说明 22-24/25
  • WGK Germany 3
  • RTECS号HP1093575
MSDS信息
(-)-MK801MALEATE供应商更多
  • 公司名称:上海波以尔化工有限公司
  • 联系电话:
  • 产品介绍: 英文名称:(-)-MK 801 Maleate
    CAS:121917-57-5
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  • 公司名称:武汉易泰科技有限公司上海分公司
  • 联系电话:86-21-50328103 * 801、802、803、804 Mobile:18930552037
  • 产品介绍: 英文名称:(-)-MK-801 MALEATE
    CAS:121917-57-5
    纯度:99% HPLC 包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
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  • 公司名称:芷威(上海)化学科技有限公司
  • 联系电话:021-20221225;13917446399;QQ:2381298399
  • 产品介绍: 英文名称:(-)-MK801MALEATE
    CAS:121917-57-5
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  • 公司名称:大连美仑生物技术有限公司
  • 联系电话:0411-66771943;0411-66771942
  • 产品介绍: 英文名称:(-)-MK 801 Maleate
    CAS:121917-57-5
    纯度:>98%,BR 包装信息:430RMB/10MG 备注:1380
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  • 公司名称:上海皓元医药股份有限公司
  • 联系电话:86-21-58998985
  • 产品介绍: 英文名称:(-)-MK 801 (Maleate)
    CAS:121917-57-5
    纯度:>98% 包装信息:465RMB/10mg 备注:试剂级
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"(-)-MK801MALEATE"相关产品信息