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簡(jiǎn)要描述：（+）MK-801 maleate 77086-22-7Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM
產(chǎn)品型號(hào)：廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2026-02-25訪 問(wèn) 量：1655產(chǎn)品分類(lèi)
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 77086-22-7 |
|---|---|---|---|
| 分子式 | C20H19NO4 | 純度 | ＞98% |
| 分子量 | 337.37 | 貨號(hào) | abs810777 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a potent N-methyl-D-aspartate (NMDA) | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
（+）MK-801 maleate 77086-22-7
| 產(chǎn)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 |
| 純度 | >98% |
| 儲(chǔ)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 | |
| 別名 | Dizocilpine maleate; Dizocilpine hydrogen maleate; (+)-MK 801; MK 801; MK801 |
| 外觀 | 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 | |
| 靶點(diǎn) | NMDA receptor |
| In vitro(體外研究) | 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(體內(nèi)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. |
| 參考文獻(xiàn) | |
| 參考文獻(xiàn) | [1]. Wong EH, et al. Proc Natl Acad Sci U S A, 1986, 83(18), 7104-7108. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | Neuroscience Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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