Catalog Number: 0924
Alternate Names: Dizocilpine
Chemical Name: (5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate
Biological Activity
A potent, selective and non-competitive NMDA receptor antagonist. Acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca2+ flux. An effective anti-ischemic agent in several animal models.

Available as part of the Mixed NMDA Receptor Tocriset™. (-)-enantiomer also available.

Technical Data
  • M.Wt:
    337.37
  • Formula:
    C16H15N.C4H4O4
  • Solubility:
    Soluble to 25 mM in water and to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at RT
  • CAS No:
    77086-22-7
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Other Product-Specific Information:
Background References
  1. The neuroprotective action of dizocilpine (MK-801) in the rat middle cerebral artery occlusion model of focal ischaemia.
    Gill et al.
    Br.J.Pharmacol., 1991;103:2030
  2. The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model.
    Hatfield et al.
    Eur.J.Pharmacol., 1992;216:1
  3. The anticonvulsant MK 801 is a potent N-methyl-D-aspartate antagonist.
    Wong et al.
    Proc.Natl.Acad.Sci.U.S.A., 1986;83:7104
  4. Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP.
    Zajaczkowski et al.
    Neuropharmacology, 1997;36:961
Citations:

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

54 Citations: Showing 1 - 10
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  1. Differential Somatic Ca2+ Channel Profile in Midbrain Dopaminergic Neurons
    Authors: Philippart Et al.
    The Journal of Neuroscience 2016;6:7234
  2. Glutathione-Induced Calcium Shifts in Chick Retinal Glial Cells.
    Authors: Freitas Et al.
    PLoS One 2016;11:e0153677
  3. Altered neuronal excitability underlies impaired hippocampal function in an animal model of psychosis.
    Authors: Grüter Et al.
    J Biol Chem 2015;9:117
  4. α-1 adrenoreceptors modulate GABA release onto ventral tegmental area dopamine neurons.
    Authors: Velásquez-Martínez Et al.
    BMC Neurosci 2015;88:110
  5. 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
  6. Miro1 deficiency in amyotrophic lateral sclerosis.
    Authors: Zhang Et al.
    Cell Death Dis 2015;7:100
  7. 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
  8. Calcium flux-independent NMDA receptor activity is required for Aβ oligomer-induced synaptic loss.
    Authors: Birnbaum Et al.
    J Clin Invest 2015;6:e1791
  9. 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
  10. Synaptic NMDA receptor activity is coupled to the transcriptional control of the glutathione system.
    Authors: Baxter Et al.
    Neuroscience 2015;6:6761
  11. 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
  12. 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
  13. 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
  14. MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons.
    Authors: Wang Et al.
    Nat Commun 2015;290:168
  15. 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
  16. 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
  17. FTY720 attenuates excitotoxicity and neuroinflammation.
    Authors: Cipriani Et al.
    Curr Mol Med 2015;12:86
  18. Decreased Expression of DREAM Promotes the Degeneration of Retinal Neurons.
    Authors: Chintala Et al.
    Front Aging Neurosci 2015;10:e0127776
  19. Glucocorticoid receptor gene inactivation in dopamine-innervated areas selectively decreases behavioral responses to amphetamine.
    Authors: Parnaudeau Et al.
    Front Behav Neurosci 2014;8:35
  20. Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala.
    Authors: Mirante Et al.
    J Neurosci 2014;7:62
  21. 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
  22. 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
  23. Deranged NMDAergic cortico-subthalamic transmission underlies parkinsonian motor deficits.
    Authors: Pan Et al.
    J Neuroinflammation 2014;124:4629
  24. NMDA-receptor activation but not ion flux is required for amyloid-β induced synaptic depression.
    Authors: Tamburri Et al.
    PLoS One 2013;8:e65350
  25. HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity.
    Authors: Vicente-Sánchez Et al.
    Mol Brain 2013;6:42
  26. 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
  27. Neuregulin and BDNF induce a switch to NMDA receptor-dependent myelination by oligodendrocytes.
    Authors: Lundgaard Et al.
    PLoS Biol 2013;11:e1001743
  28. Potentiation of NMDA receptor-dependent cell responses by extracellular high mobility group box 1 protein.
    Authors: Pedrazzi Et al.
    PLoS One 2012;7:e44518
  29. 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
  30. 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
  31. Glutamate controls tPA recycling by astrocytes, which in turn influences glutamatergic signals.
    Authors: Cassé Et al.
    J Neurosci 2012;32:5186
  32. Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons.
    Authors: Kaufman Et al.
    FASEB J 2012;32:3992
  33. Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity.
    Authors: Gaamouch Et al.
    J Neurosci 2012;32:10767
  34. Intrinsic modulators of auditory thalamocortical transmission.
    Authors: Lee and Sherman
    Hear Res 2012;287:43
  35. Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1.
    Authors: Straub Et al.
    Nat Neurosci 2011;14:866
  36. Suppression of the intrinsic apoptosis pathway by synaptic activity.
    Authors: Léveillé Et al.
    J Neurosci 2010;30:2623
  37. 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
  38. Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways.
    Authors: Roselli Et al.
    PLoS One 2009;4:e6011
  39. Mechanism of differential control of NMDA receptor activity by NR2 subunits.
    Authors: Gielen Et al.
    J Cereb Blood Flow Metab 2009;459:703
  40. Necrotic neurons enhance microglial neurotoxicity through induction of glutaminase by a MyD88-dependent pathway.
    Authors: Pais Et al.
    J Neurosci 2008;5:43
  41. 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
  42. Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors.
    Authors: Léveillé Et al.
    FASEB J 2008;22:4258
  43. 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
  44. Increased thalamocortical synaptic response and decreased layer IV innervation in GAP-43 knockout mice.
    Authors: Albright Et al.
    J Neurophysiol 2007;98:1610
  45. 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
  46. Vasoconstrictive neurovascular coupling during focal ischemic depolarizations.
    Authors: Shin Et al.
    J Cereb Blood Flow Metab 2006;26:1018
  47. D-serine is the dominant endogenous coagonist for NMDA receptor neurotoxicity in organotypic hippocampal slices.
    Authors: Shleper Et al.
    Nature 2005;25:9413
  48. Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons.
    Authors: Calò Et al.
    J Neurosci 2005;25:2245
  49. Brain-derived neurotrophic factor mRNA and protein are targeted to discrete dendritic laminas by events that trigger epileptogenesis.
    Authors: Tongiorgi Et al.
    J Neurosci 2004;24:6842
  50. 2,7-Bis-(4-amidinobenzylidene)-cycloheptan-1-one dihydrochloride, tPA stop, prevents tPA-enhanced excitotoxicity both in vitro and in vivo.
    Authors: Liot Et al.
    Proc Natl Acad Sci U S A 2004;24:1153
  51. Angiopoietin-1-induced PI3-kinase activation prevents neuronal apoptosis.
    Authors: Valable Et al.
    Oncotarget 2003;17:443
  52. Transforming growth factor alpha-induced expression of type 1 plasminogen activator inhibitor in astrocytes rescues neurons from excitotoxicity.
    Authors: Gabriel Et al.
    FASEB J 2003;17:277
  53. Glutamate antagonists limit tumor growth.
    Authors: Rzeski Et al.
    J Neurosci 2001;98:6372
  54. Enhancement of glutamate release by L-fucose changes effects of glutamate receptor antagonists on long-term potentiation in the rat hippocampus.
    Authors: Matthies Et al.
    Learn Mem 2000;7:227
Expand to show all 54 Citations

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