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| 品牌 | absin | CAS | 77086-22-7 |
|---|---|---|---|
| 分子式 | C20H19NO4 | 纯度 | ＞98% |
| 分子量 | 337.37 | 货号 | abs810777 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is a potent N-methyl-D-aspartate (NMDA) | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
（+）MK-801 maleate 77086-22-7
| 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. |
| 研究领域 | |
| 研究领域 | Neuroscience Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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