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

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Images

Chemical Structure - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027), expandable thumbnail
  • Functional Studies - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (AB120027), expandable thumbnail

Publications

Key facts

CAS number
77086-22-7
Purity
> 99%
Form
Solid
Molecular weight
337.4 Da
Molecular formula
C20H19NO4
PubChem identifier
6420042
Nature
Synthetic

Alternative names

Recommended products

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

Key facts

Purity
> 99%
PubChem identifier
6420042
Biochemical name
Dizocilpine maleate
Biological description

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

Canonical SMILES
CC12C3=CC=CC=C3CC(N1)C4=CC=CC=C24.C(=CC(=O)O)C(=O)O
Isomeric 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 name
(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

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary info

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

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.

Associated diseases and disorders

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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2 product images

  • Chemical Structure - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (ab120027), expandable thumbnail

    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

  • Functional Studies - (+)-MK 801 maleate (Dizocilpine), Non-competitive NMDA antagonist (ab120027), expandable thumbnail
    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.

    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).

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