(+)-MK 801 maleate

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(+)-MK 801 maleate | CAS No. 77086-22-7 | NMDA Receptor Antagonists
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Description: Non-competitive NMDA antagonist; acts at ion channel site
Alternative Names: Dizocilpine

Chemical Name: (5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate

Purity: ≥99%

Product Details
Citations (91)

Biological Activity

(+)-MK 801 maleate is a high affinity (Ki = 37.2 nM), selective and non-competitive NMDA receptor antagonist. (+)-MK 801 maleate acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux. It is an effective anti-ischemic agent in several animal models. (+)-MK 801 maleate increases motor activity in rat models. (+)-MK 801 maleate inhibits proliferation and increases apoptosis in hippocampal neural stem cells (NSCs). (+)-MK 801 maleate induces schizophrenia-like symptoms in rodents.

(-)-enantiomer also available.

Technical Data

Soluble to 20 mM in water with gentle warming and to 100 mM in DMSO
Store at RT

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Other Product-Specific Information:

Background References

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  2. Functional Indicators of Glutamate Transport in Single Striatal Astrocytes and the Influence of Kir4.1 in Normal and Huntington Mice

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  6. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
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  7. Calpain-mediated degradation of MDMx/MDM4 contributes to HIV-induced neuronal damage.
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  8. Potentiation of NMDA receptor-dependent cell responses by extracellular high mobility group box 1 protein.
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  9. Chronic Stress-induced Behavioral Changes Associated with Subregion Selective Serotonin Cell Death in the Dorsal Raphe
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  10. The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model.
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  12. The anticonvulsant MK 801 is a potent N-MthD.-aspartate antagonist.
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  13. Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP.
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  14. Effects of dizocilpine (MK-801) on motor activity and memory.
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  15. Effect of NMDA on proliferation and apoptosis in hippocampal neural stem cells treated with MK-801.
    Ding et al.
    Exp.Ther.Med., 2018;16:1137

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Citations for (+)-MK 801 maleate

The citations listed below are publications that use Tocris products. Selected citations for (+)-MK 801 maleate include:

91 Citations: Showing 1 - 10

  1. NMDAR-Activated PP1 Dephosphorylates GluN2B to Modulate NMDAR Synaptic Content.
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    Cell Rep  2019;28:332
  2. Time-dependent alterations in the expression of NMDA receptor subunits along the dorsoventral hippocampal axis in an animal model of nascent psychosis.
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    ACS.Chem.Neurosci.  2018;9:2241
  3. AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation.
    Authors: Marinangeli Et al.
    iScience  2018;9:1
  4. Activity-Dependent Downscaling of Subthreshold Synaptic Inputs during Slow-Wave-Sleep-like Activity In Vivo.
    Authors: González-Rueda Et al.
    Neuron  2018;97:1244
  5. Electrophysiological measurement of ion channels on plasma/organelle membranes using an on-chip lipid bilayer system.
    Authors: Kamiya Et al.
    Sci Rep  2018;8:17498
  6. The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences.
    Authors: McKay Et al.
    Cell Rep  2018;25:841
  7. DA Cells Differentially Regulate Striatal Cholinergic Transmission across Regions through Corelease of DA and Glutamate.
    Authors: Cai and Ford
    Cell Rep  2018;25:3148
  8. Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice.
    Authors: Sánchez-Blázquez Et al.
    Int J Neuropsychopharmacol  2018;21:938
  9. Neuronal Activity-Dependent Activation of Astroglial Calcineurin in Mouse Primary Hippocampal Cultures.
    Authors: Lim Et al.
    Int J Mol Sci  2018;19
  10. Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling.
    Authors: Brancaccio Et al.
    Neuron  2017;93:1420
  11. A novel crosstalk within the endocannabinoid system controls GABA transmission in the striatum.
    Authors: Musella
    Sci Rep  2017;7(1):7363
  12. Differential Somatic Ca2+ Channel Profile in Midbrain DArgic Neurons
    Authors: Philippart Et al.
    The Journal of Neuroscience  2016;6:7234
  13. Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes.
    Authors: O'Donnell Et al.
    J Neurosci  2016;36:7109
  14. Glutathione-Induced Calcium Shifts in Chick Retinal Glial Cells.
    Authors: Freitas Et al.
    PLoS One  2016;11:e0153677
  15. Altered neuronal excitability underlies impaired hippocampal function in an animal model of psychosis.
    Authors: Grüter Et al.
    J Biol Chem  2015;9:117
  16. α-1 adrenoreceptors modulate GABA release onto ventral tegmental area DA neurons.
    Authors: Velásquez-Martínez Et al.
    BMC Neurosci  2015;88:110
  17. Functional plasticity of GAT-3 in avian Müller cells is regulated by neurons via a glutamatergic input.
    Authors: Schitine Et al.
    PLoS One  2015;82:42
  18. Miro1 deficiency in amyotrophic lateral sclerosis.
    Authors: Zhang Et al.
    Cell Death Dis  2015;7:100
  19. Conformations of tissue plasminogen activator (tPA) orchestrate neuronal survival by a crosstalk between EGFR and NMDAR.
    Authors: Bertrand Et al.
    Cell Death Dis  2015;6:e1924
  20. Calcium flux-independent NMDA receptor activity is required for Aβ oligomer-induced synaptic loss.
    Authors: Birnbaum Et al.
    J Clin Invest  2015;6:e1791
  21. Brain ischemia downregulates the neuroprotective GDNF-Ret signaling by a calpain-dependent mechanism in cultured hippocampal neurons.
    Authors: Curcio Et al.
    J Neurosci  2015;6:e1645
  22. Synaptic NMDA receptor activity is coupled to the transcriptional control of the glutathione system.
    Authors: Baxter Et al.
    Neuroscience  2015;6:6761
  23. The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders.
    Authors: Rodríguez-Muñoz Et al.
    Int J Neuropsychopharmacol  2015;6:35458
  24. Miro1 Regulates Activity-Driven Positioning of Mitochondria within Astrocytic Processes Apposed to Synapses to Regulate Intracellular Calcium Signaling.
    Authors: Stephen Et al.
    Front Behav Neurosci  2015;35:15996
  25. Rewarding Effects of Optical Stimulation of Ventral Tegmental Area Glutamatergic Neurons.
    Authors: Wang Et al.
    J Neurosci  2015;35:15948
  26. Oligodendrocytes Are Targets of HIV-1 Tat: NMDA and AMPA Receptor-Mediated Effects on Survival and Development.
    Authors: Zou Et al.
    J Neurosci  2015;35:11384
  27. MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons.
    Authors: Wang Et al.
    Nat Commun  2015;290:168
  28. Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia.
    Authors: Quillinan Et al.
    Neuropharmacology  2015;284:555
  29. Neurobehavioral Differences Between Mice Receiving Distinct Neuregulin Variants as Neonates; Impact on Sensitivity to MK-801.
    Authors: Kato Et al.
    Cell Death Dis  2015;15:222
  30. FTY720 attenuates excitotoxicity and neuroinflammation.
    Authors: Cipriani Et al.
    Curr Mol Med  2015;12:86
  31. Activity-dependent differences in function between proximal and distal Schaffer collaterals.
    Authors: Owen and Grover
    J Neurophysiol  2015;113:3646
  32. Decreased Expression of DREAM Promotes the Degeneration of Retinal Neurons.
    Authors: Chintala Et al.
    Front Aging Neurosci  2015;10:e0127776
  33. Glucocorticoid receptor gene inactivation in DA-innervated areas selectively decreases behavioral responses to amphetamine.
    Authors: Parnaudeau Et al.
    Front Behav Neurosci  2014;8:35
  34. Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala.
    Authors: Mirante Et al.
    J Neurosci  2014;7:62
  35. β-amyloid induces a dying-back process and remote trans-synaptic alterations in a microfluidic-based reconstructed neuronal network.
    Authors: Deléglise Et al.
    Acta Neuropathol Commun  2014;2:145
  36. The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases.
    Authors: Sánchez-Blázquez Et al.
    Neurochem Int  2014;17:1943
  37. Deranged NMDAergic cortico-subthalamic transmission underlies parkinsonian motor deficits.
    Authors: Pan Et al.
    J Neuroinflammation  2014;124:4629
  38. NMDA-receptor activation but not ion flux is required for amyloid-β induced synaptic depression.
    Authors: Tamburri Et al.
    PLoS One  2013;8:e65350
  39. Activation of group I metabotropic glutamate receptors potentiates heteromeric kainate receptors.
    Authors: Rojas Et al.
    Mol Pharmacol  2013;83:106
  40. HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity.
    Authors: Vicente-Sánchez Et al.
    Mol Brain  2013;6:42
  41. Impaired glutamate recycling and GluN2B-mediated neuronal calcium overload in mice lacking TGF-β1 in the CNS.
    Authors: Koeglsperger Et al.
    Glia  2013;61:985
  42. Calcium responses to synaptically activated bursts of action potentials and their synapse-independent replay in cultured networks of hippocampal neurons.
    Authors: Bengtson Et al.
    Biochim Biophys Acta  2013;1833:1672
  43. Non-Hebbian plasticity at C-fiber synapses in rat spinal cord lamina I neurons.
    Authors: Naka Et al.
    Pain  2013;154:1333
  44. Enhanced expression of WD repeat-containing protein 35 (WDR35) stimulated by domoic acid in rat hippocampus: involvement of reactive oxygen species generation and p38 mitogen-activated protein kinase activation.
    Authors: Tsunekawa Et al.
    J Neuroinflammation  2013;14:4
  45. Neuregulin and BDNF induce a switch to NMDA receptor-dependent myelination by oligodendrocytes.
    Authors: Lundgaard Et al.
    PLoS Biol  2013;11:e1001743
  46. A modulatory effect of the feedback from higher visual areas to V1 in the mouse.
    Authors: Pasquale and Sherman
    J Neurophysiol  2013;109:2618
  47. Duodenal lipid sensing activates vagal afferents to regulate non-shivering brown fat thermogenesis in rats.
    Authors: Blouet and Schwartz
    PLoS One  2012;7:e51898
  48. Genetic inhibition of CaMKII in dorsal striatal medium spiny neurons reduces functional excitatory synapses and enhances intrinsic excitability.
    Authors: Klug Et al.
    PLoS One  2012;7:e45323
  49. Potentiation of NMDA receptor-dependent cell responses by extracellular high mobility group box 1 protein.
    Authors: Pedrazzi Et al.
    PLoS One  2012;7:e44518
  50. Differences in spontaneously avoiding or approaching mice reflect differences in CB1-mediated signaling of dorsal striatal transmission.
    Authors: Laricchiuta Et al.
    PLoS One  2012;7:e33260
  51. The mu-opioid receptor and the NMDA receptor associate in PAG neurons: implications in pain control.
    Authors: Rodríguez-Muñoz Et al.
    Neuropsychopharmacology  2012;37:338
  52. State-dependent increase of cortical gamma activity during REM sleep after selective blockade of NR2B subunit containing NMDA receptors.
    Authors: Kocsis
    Sleep  2012;35:1011
  53. Glutamate controls tPA recycling by astrocytes, which in turn influences glutamatergic signals.
    Authors: Cassé Et al.
    J Neurosci  2012;32:5186
  54. Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons.
    Authors: Kaufman Et al.
    FASEB J  2012;32:3992
  55. Parasynaptic NMDA receptor signaling couples neuronal glutamate transporter function to AMPA receptor synaptic distribution and stability.
    Authors: Jarzylo and Man
    J Neurosci  2012;32:2552
  56. Endocannabinoid-mediated long-term depression of afferent excitatory synapses in hippocampal pyramidal cells and GABAergic interneurons.
    Authors: Peterfi Et al.
    J Neurosci  2012;32:14448
  57. Interleukin-1β causes anxiety by interacting with the endocannabinoid system.
    Authors: Rossi Et al.
    J Neurosci  2012;32:13896
  58. Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity.
    Authors: Gaamouch Et al.
    J Neurosci  2012;32:10767
  59. Pharmacological evidence that D-aspartate activates a current distinct from ionotropic glutamate receptor currents in Aplysia californica.
    Authors: Carlson Et al.
    Brain Behav  2012;2:391
  60. Intrinsic modulators of auditory thalamocortical transmission.
    Authors: Lee and Sherman
    Hear Res  2012;287:43
  61. Decreased afferent excitability contributes to synaptic depression during high-frequency stimulation in hippocampal area CA1.
    Authors: Kim Et al.
    J Neurophysiol  2012;108:1965
  62. CDK5 is essential for soluble amyloid β-induced degradation of GKAP and remodeling of the synaptic actin cytoskeleton.
    Authors: Roselli Et al.
    PLoS One  2011;6:e23097
  63. Pyramidal neurons are "neurogenic hubs" in the neurovascular coupling response to whisker stimulation.
    Authors: Lecrux Et al.
    J Neurosci  2011;31:9836
  64. Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1.
    Authors: Straub Et al.
    Nat Neurosci  2011;14:866
  65. Glutamatergic mechanisms for speed control and network operation in the rodent locomotor CpG.
    Authors: Talpalar and Kiehn
    Front Neural Circuits  2010;4
  66. Suppression of the intrinsic apoptosis pathway by synaptic activity.
    Authors: Léveillé Et al.
    J Neurosci  2010;30:2623
  67. Rapid activation of dormant presynaptic terminals by phorbol esters.
    Authors: Chang Et al.
    J Neurosci  2010;30:10048
  68. Na+ mechanism of delta-opioid receptor induced protection from anoxic K+ leakage in the cortex.
    Authors: Chao Et al.
    Cell Mol Life Sci  2009;66:1105
  69. Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways.
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    PLoS One  2009;4:e6011
  70. Mechanism of differential control of NMDA receptor activity by NR2 subunits.
    Authors: Gielen Et al.
    J Cereb Blood Flow Metab  2009;459:703
  71. Clovamide and rosmarinic acid induce neuroprotective effects in in vitro models of neuronal death.
    Authors: Fallarini Et al.
    Br J Pharmacol  2009;157:1072
  72. Necrotic neurons enhance microglial neurotoxicity through induction of glutaminase by a MyD88-dependent pathway.
    Authors: Pais Et al.
    J Neurosci  2008;5:43
  73. Cortical adenylyl cyclase 1 is required for thalamocortical synapse maturation and aspects of layer IV barrel development.
    Authors: Iwasato Et al.
    J Neurosci  2008;28:5931
  74. Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors.
    Authors: Léveillé Et al.
    FASEB J  2008;22:4258
  75. A quantitative assessment of glutamate uptake into hippocampal synaptic terminals and astrocytes: new insights into a neuronal role for excitatory amino acid transporter 2 (EAAT2).
    Authors: Furness Et al.
    Neuroscience  2008;157:80
  76. Increased thalamocortical synaptic response and decreased layer IV innervation in GAP-43 knockout mice.
    Authors: Albright Et al.
    J Neurophysiol  2007;98:1610
  77. PREGS induces LTP in the hippocampal dentate gyrus of adult rats via the tyrosine phosphorylation of NR2B coupled to ERK/CREB [corrected] signaling.
    Authors: Chen Et al.
    J Neurophysiol  2007;98:1538
  78. Plasticity of intrinsic excitability during long-term depression is mediated through mGluR-dependent changes in I(h) in hippocampal CA1 pyramidal neurons.
    Authors: Brager and Johnston
    J Neurosci  2007;27:13926
  79. A form of perforant path LTP can occur without ERK1/2 phosphorylation or immediate early gene induction.
    Authors: Steward Et al.
    Learn Mem  2007;14:433
  80. Activation of NMDA receptors increases proliferation and differentiation of hippocampal neural progenitor cells.
    Authors: Joo Et al.
    J Cell Sci  2007;120:1358
  81. Vasoconstrictive neurovascular coupling during focal ischemic depolarizations.
    Authors: Shin Et al.
    J Cereb Blood Flow Metab  2006;26:1018
  82. Glutaric acid and its metabolites cause apoptosis in immature oligodendrocytes: a novel mechanism of white matter degeneration in glutaryl-CoA dehydrogenase deficiency.
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    Pediatr Res  2005;57:771
  83. D-serine is the dominant endogenous coagonist for NMDA receptor neurotoxicity in organotypic hippocampal slices.
    Authors: Shleper Et al.
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  84. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
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    J Neurosci  2005;25:2245
  85. Brain-derived neurotrophic factor mRNA and protein are targeted to discrete dendritic laminas by events that trigger epileptogenesis.
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    J Neurosci  2004;24:6842
  86. 2,7-Bis-(4-amidinobenzylidene)-cycloheptan-1-one dihydrochloride, tPA stop, prevents tPA-enhanced excitotoxicity both in vitro and in vivo.
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  87. Angiopoietin-1-induced PI3-kinase activation prevents neuronal apoptosis.
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  88. Transforming growth factor alpha-induced expression of type 1 plasminogen activator inhibitor in astrocytes rescues neurons from excitotoxicity.
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  89. Development of a human neuronal cell model for human immunodeficiency virus (HIV)-infected macrophage-induced neurotoxicity: apoptosis induced by HIV type 1 primary isolates and evidence for involvement of the Bcl-2/Bcl-xL-sensitive intrinsic apoptosis pa
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  90. Glutamate antagonists limit tumor growth.
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    Learn Mem  2000;7:227


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