AB120027

(+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist

Name: (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA拮抗剂 (ab120027)| Abcam中文官网
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SKU: AB120027
Price: 859 CNY
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(42 Publications)

MW 337.4 Da, Purity >99%. Potent, selective non-competitive NMDA receptor antagonist. Open channel blocker of the NMDA receptor operated ion channel.

查看别名

AMPA 1, AMPA-selective glutamate receptor 1, AW490526, EB11, EIEE27, EPND, FESD, GLUH1, GRIA1_HUMAN, GRIN 2A, GRIN 2B, GRIN3A, GRIN3B, GluA1, GluN1, GluN2A, GluN2C, GluN2D, GluR-1, GluR-A, GluR-K1, Glutamate Receptor Ionotropic N Methyl D Aspartate 2B, Glutamate Receptor Ionotropic N Methyl D Aspartate 2C, Glutamate Receptor Ionotropic N Methyl D Aspartate subunit 2B, Glutamate Receptor Ionotropic N methyl D aspartate 3A, Glutamate [NMDA] receptor subunit epsilon-1, Glutamate [NMDA] receptor subunit epsilon-2, Glutamate [NMDA] receptor subunit epsilon-3, Glutamate [NMDA] receptor subunit epsilon-4, Glutamate [NMDA] receptor subunit zeta-1, Glutamate receptor, Glutamate receptor 1, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, Glutamate receptor ionotropic N methyl D aspartate 1, Glutamate receptor ionotropic N methyl D aspartate 2A, Glutamate receptor ionotropic N methyl D aspartate 3B, Glutamate receptor ionotropic NMDA2B, Glutamate receptor ionotropic, N-methyl-D aspartate, subunit 1, Glutamate receptor ionotropic, NMDA 2C, Glutamate receptor subunit epsilon 2, Glutamate receptor, ionotropic, N-methyl D-aspartate 2D, Glutamate receptor, ionotropic, NMDA2B (epsilon 2), Grin2c, Grin2d, HBGR1, LKS, MGC133252, MGC142178, MGC142180, MRD6, MRD8, N Methly D Aspartate Receptor Channel Subunit Epsilon 3, N methyl D asparate receptor channel subunit epsilon 2, N methyl D aspartate receptor channel subunit zeta 1, N methyl D aspartate receptor channel, subunit epsilon 1, N methyl D aspartate receptor subunit 2A, N methyl D aspartate receptor subunit 2B, N methyl D aspartate receptor subunit 2C, N methyl d aspartate receptor subunit 2D, N-methyl D-aspartate receptor subtype 2A, N-methyl D-aspartate receptor subtype 2B, N-methyl D-aspartate receptor subtype 2C, N-methyl D-aspartate receptor subtype 2D, N-methyl-D-aspartate receptor, N-methyl-D-aspartate receptor subunit 3, N-methyl-D-aspartate receptor subunit NR1, NMD-R1, NMDA 1, NMDA 2D, NMDA NR2B, NMDA receptor 1, NMDA receptor subtype 2A, NMDA receptor subunit 3A, NMDA receptor subunit 3B, NMDAR, NMDAR2C, NMDAR2D, NMDE1_HUMAN, NMDE2_HUMAN, NMDE3_HUMAN, NMDE4_HUMAN, NMDZ1_HUMAN, NR1, NR2A, NR2B, NR2C, NR2D, NR3, OTTHUMP00000041930, OTTHUMP00000160135, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000174531, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243, estrogen receptor binding CpG island, glutamate receptor ionotropic NMDA 2D, glutamate receptor ionotropic, NMDA 1, hNR 3, hNR2A

2 Images

Functional Studies - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027)

FuncS

PubMed

Functional Studies - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027)

CDPPB does not influence spontaneous locomotor activity but attenuates MK-801-induced hyperlocomotion. Animals were injected (s.c./i.p.) with PBS/Vehicle (0/0), 0.2 mg/kg MK-801/Vehicle (0.2/0), 0.2 mg/kg MK-801/3 mg/kg CDPPB (0.2/3) or 0.2 mg/kg MK-801/10 mg/kg CDPPB (0.2/10) 20 minutes before being placed in the activity chamber. Activity was recorded for 30 minutes. Data are expressed as mean ± SEM of distance traveled (n=6-7). **p<0.01 vs. 0.2 mg/kg MK-801/Vehicle group (One-way ANOVA, Bonferroni's posttest).

Image from Fowler SW et al., Neurobiol Learn Mem. 2010;95(1):73-9. Fig 2(B).; doi: 10.1016/j.nlm.2010.11.009 with permission from Elsevier.

Chemical Structure - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027)

Chemical Structure

Lab

Chemical Structure - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027)

2D chemical structure image of ab120027, (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist

关键信息

CAS 号

77086-22-7

纯度

>99%

形式

Solid

form

分子量

337.4 Da

分子式

C20H19NO4

PubChem

6420042

属性

Synthetic

生化试剂名称

Dizocilpine maleate

生物学描述

Potent, selective non-competitive NMDA receptor antagonist. Open channel blocker of the NMDA receptor operated ion channel.

经典 SMILES

CC12C3=CC=CC=C3CC(N1)C4=CC=CC=C24.C(=CC(=O)O)C(=O)O

同分异构的 SMILES

C[C@@]12C3=CC=CC=C3C[C@@H](N1)C4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O

InChi

InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-,16+;/m1./s1

InChiKey

QLTXKCWMEZIHBJ-PJGJYSAQSA-N

IUPAC 名

(Z)-but-2-enedioic acid;(1S,9R)-1-methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaene

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性能和储存信息

运输条件

Ambient - Can Ship with Ice

储存信息

Store under desiccating conditions|The product can be stored for up to 12 months

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补充信息

This supplementary information is collated from multiple sources and compiled automatically.

NMDAR2A NMDAR2B GluN2C NMDAR1 Glutamate Receptor 1 (AMPA subtype) NMDAR3A + 3B and GluN2D are subunits of ionotropic glutamate receptors specifically the N-methyl-D-aspartate (NMDA) receptor and AMPA receptor subtypes. These receptors are integral membrane proteins involved in synaptic transmission and plasticity. NMDA receptors which include these subunits form a tetrameric structure typically composed of two GluN1 and two GluN2 or GluN3 subunits. The mass of each subunit varies but GluN1 has an approximate molecular weight of 120 kDa. These receptors are primarily expressed in the central nervous system within the neuronal synapses modulating excitatory neurotransmission.

Biological function summary

These receptor subunits play an important role in synaptic plasticity memory and learning by mediating calcium ion influx in response to glutamate binding. They form part of a complex that includes auxiliary proteins that modulate their function and pharmacology. NMDAR subunits assemble to establish functional NMDA receptors requiring co-agonists such as glycine or D-serine and distinguished by their dependence on membrane depolarization to remove the Mg²⁺ block. Meanwhile AMPA receptors through the GluR1 subunit rapidly mediate excitatory postsynaptic potentials.

Pathways

NMDARs and associated subunits participate significantly in the long-term potentiation (LTP) and long-term depression (LTD) pathways essential for synaptic strengthening and weakening. These synaptic plasticity pathways heavily involve signaling proteins such as calcium/calmodulin-dependent protein kinase II (CaMKII) and protein kinase C (PKC). Furthermore the interaction with neuronal nitric oxide synthase (nNOS) links NMDAR activity to downstream signaling cascades which can influence synaptic strength and neuronal health.

Aberrations in NMDA receptor function are implicated in neurological conditions such as Alzheimer's disease and schizophrenia. Reduced NMDAR activity is associated with cognitive decline and synaptic dysfunction in Alzheimer's partly due to interactions with amyloid-beta proteins. In schizophrenia altered expression of NMDAR subunits especially NMDA antagonists like MK-801 and DL-AP5 hint at a dysregulated glutamatergic system contributing to symptoms. Addressing these pathways and interactions provides a foundation for developing therapeutic strategies.

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产品实验方案

Visit the General protocols
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文献 (42)

Recent publications for all applications. Explore the full list and refine your search

European archives of psychiatry and clinical neuroscience 274:1013-1019 PubMed37934233

2023

Psilocybin does not induce the vulnerability marker HSP70 in neurons susceptible to Olney's lesions.

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Species

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Ana-Maria Iorgu,Andrei-Nicolae Vasilescu,Natascha Pfeiffer,Rainer Spanagel,Anne Stephanie Mallien,Dragos Inta,Peter Gass

International journal of molecular sciences 23: PubMed35408792

2022

Clozapine Increases Nestin Concentration in the Adult Male Rat Hippocampus: A Preliminary Study.

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Hakan Kayir,Bryan W Jenkins,Begüm Alural,Jibran Y Khokhar

Frontiers in behavioral neuroscience 15:815713 PubMed35095443

2022

Behavioral and Neuroanatomical Consequences of Cell-Type Specific Loss of Dopamine D2 Receptors in the Mouse Cerebral Cortex.

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Gloria S Lee,Devon L Graham,Brenda L Noble,Taylor S Trammell,Deirdre M McCarthy,Lisa R Anderson,Marcelo Rubinstein,Pradeep G Bhide,Gregg D Stanwood

eNeuro 8: PubMed34862204

2021

Drug-Induced Hyperglycemia as a Potential Contributor to Translational Failure of Uncompetitive NMDA Receptor Antagonists.

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Eric Yuhsiang Wang,Ted Weita Lai

Cell reports 36:109496 PubMed34348150

2021

Slow AMPA receptors in hippocampal principal cells.

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Niccolò P Pampaloni,Irene Riva,Anna L Carbone,Andrew J R Plested

Frontiers in cellular neuroscience 14:74 PubMed32300294

2020

Astrocytes Are Required for Oligodendrocyte Survival and Maintenance of Myelin Compaction and Integrity.

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Reshmi Tognatta,Molly T Karl,Sharyl L Fyffe-Maricich,Anastas Popratiloff,Eric D Garrison,Jessica K Schenck,Mohammad Abu-Rub,Robert H Miller

PloS one 15:e0229499 PubMed32126102

2020

Hypothermia but not NMDA receptor antagonism protects against stroke induced by distal middle cerebral arterial occlusion in mice.

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Species

Unspecified reactive species

Che-Wei Liu,Kate Hsiurong Liao,Hsin Tseng,Ching Mei Wu,Hsiao-Yun Chen,Ted Weita Lai

Reproductive sciences (Thousand Oaks, Calif.) 27:916-924 PubMed31933163

2020

Nicotine Suppresses the Invasiveness of Human Trophoblasts by Downregulation of CXCL12 Expression through the Alpha-7 Subunit of the Nicotinic Acetylcholine Receptor.

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Jing Chen,Min Qiu,Zirui Huang,Jimei Chen,Chengbin Zhou,Fengzhen Han,Yanji Qu,Sheng Wang,Jian Zhuang,Xiaohong Li

Pathobiology : journal of immunopathology, molecul 86:274-284 PubMed31574524

2019

R5 HIV-1 gp120 Activates p38 MAPK to Induce Rat Cardiomyocyte Injury by the CCR5 Coreceptor.

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Rui Gao,Qiujuan Fang,Xi Zhang,Qin Xu,Hanhui Ye,Wenyan Guo,Jiao He,Yahong Chen,Ruixing Wang,Zhijuan Wu,Jing Yu

Cell reports 25:3582-3590.e4 PubMed30590034

2018

Structural Basis of the Proton Sensitivity of Human GluN1-GluN2A NMDA Receptors.

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Species

Unspecified reactive species

Jin-Bao Zhang,Shenghai Chang,Pan Xu,Miao Miao,Hangjun Wu,Youyi Zhang,Tongtong Zhang,Han Wang,Jilin Zhang,Chun Xie,Nan Song,Cheng Luo,Xing Zhang,Shujia Zhu

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(+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist