顺丁烯二酸盐 (-)-MK

中文名	(-)-MK 801 Maleate
英文名	(-)-MK 801 Maleate
别名	顺丁烯二酸盐 (-)-MK (-)-MK 801马来酸 (-)-MK801 马来酸盐
英文别名	MK801 C13737 MK 801 (-)-MK 801 (-)-MK801MALEATE (-)-MK 801 Maleate (-)-MK-801 MALEATE 5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5R,10S) (5S,10R)-(-)-5-METHYL-10,11-DIHYDRO-5H-DIBENZO[A,D]CYCLOHEPTEN-5,10-IMINE MALEATE (5R)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-butenedioate
CAS	121917-57-5
化学式	C20H19NO4
分子量	337.37
溶解度	DMSO: >20 mg/mL
存储条件	-20℃
外观	固体
颜色	white
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. 体外神经生理学研究使用大鼠皮质切片制剂，证明了dizocilpine对N-Me-D-Asp去极化响应具有有效的，选择性的，非竞争性的拮抗作用，但是对红藻氨酸或使君子氨酸无此作用。Phencyclidine，ketamine，SKF 10047，和dizocilpine的对映异构体，作为N-Me-D-Asp拮抗剂的效能与它们作为[3H] dizocilpine结合抑制剂的效能密切相关。这表明，dizocilpine结合位点与N-Me-D-Asp受体相关，并解释了dizocilpine作为抗痉挛剂的作用机制。
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. 在脊髓缺血性损伤(ISCI)后，所有对照组大鼠患有严重的永久性神经功能缺损，而dizocilpine治疗的大鼠具有统计学上(P < .05)更好的神经功能，并且恢复良好。组织病理学表明对照组大鼠的腰灰质出现严重的神经元坏死，而dizocilpine处理的大鼠仅表现出轻度损伤。这些结果表明，ISCI 之前，dizocilpine单剂量给药提供显著的神经保护作用。
安全术语	S22 - 切勿吸入粉尘。 S24/25 - 避免与皮肤和眼睛接触。
WGK Germany	3
RTECS	HP1093575

顺丁烯二酸盐 (-)-MK - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	2.964 ml	14.821 ml	29.641 ml
5 mM	0.593 ml	2.964 ml	5.928 ml
10 mM	0.296 ml	1.482 ml	2.964 ml
5 mM	0.059 ml	0.296 ml	0.593 ml

最后更新：2024-01-02 23:10:35

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产品名: (-)-MK 801 Maleate 去供应商网站查看询盘
CAS: 121917-57-5
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产品名: (-)-MK 801马来酸盐去供应商网站查看询盘
CAS: 121917-57-5
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产品描述: 中文名：(-)-MK 801马来酸盐英文名:(-)-Dizocilpine maleate CAS:121917-57-5 规格:99% 产地:中国上海

上海源叶生物科技有限公司

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产品名: (-)-MK 801 Maleate 去供应商网站查看询盘
CAS: 121917-57-5
产地: 上海
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