(+)-MK 801 maleate

Cat. No. 0924

(+)-MK 801 maleate C16H15N.C4H4O4 [77086-22-7]

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Alternative Name: 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. Part of the Mixed NMDA Receptor Tocriset™. (-)-MK 801 maleate (Cat. No. 0955) 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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Certificate of Analysis / Product Datasheet
Select another batch:

Zajaczkowski et al (1997) Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP. Neuropharmacology 36 961. PMID: 9257940.

Hatfield et al (1992) The dose-response relationship and therapeutic window for dizocilpine (MK-801) in a rat focal ischaemia model. Eur.J.Pharmacol. 216 1. PMID: 1526248.

Gill et al (1991) The neuroprotective action of dizocilpine (MK-801) in the rat middle cerebral artery occlusion model of focal ischaemia. Br.J.Pharmacol. 103 2030. PMID: 1912992.

Wong et al (1986) The anticonvulsant MK 801 is a potent N-methyl-D-aspartate antagonist. Proc.Natl.Acad.Sci.U.S.A. 83 7104. PMID: 3529096.

If you know of a relevant reference for this product please let us know.

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

Freitas et al (2016) Glutathione-Induced Calcium Shifts in Chick Retinal Glial Cells. PLoS One 11 e0153677. PMID: 27078878.

Philippart et al (2016) Differential Somatic Ca2+ Channel Profile in Midbrain Dopaminergic Neurons The Journal of Neuroscience 6 7234. PMID: 27383597.

Baxter et al (2015) Synaptic NMDA receptor activity is coupled to the transcriptional control of the glutathione system. Neuroscience 6 6761. PMID: 25854456.

Bertrand et al (2015) Conformations of tissue plasminogen activator (tPA) orchestrate neuronal survival by a crosstalk between EGFR and NMDAR. Cell Death Dis 6 e1924. PMID: 26469972.

Birnbaum et al (2015) Calcium flux-independent NMDA receptor activity is required for Aβ oligomer-induced synaptic loss. J Clin Invest 6 e1791. PMID: 26086964.

Chintala et al (2015) Decreased Expression of DREAM Promotes the Degeneration of Retinal Neurons. Front Aging Neurosci 10 e0127776. PMID: 26020793.

Cipriani et al (2015) FTY720 attenuates excitotoxicity and neuroinflammation. Curr Mol Med 12 86. PMID: 25953296.

Curcio et al (2015) Brain ischemia downregulates the neuroprotective GDNF-Ret signaling by a calpain-dependent mechanism in cultured hippocampal neurons. J Neurosci 6 e1645. PMID: 25675305.

Grüter et al (2015) Altered neuronal excitability underlies impaired hippocampal function in an animal model of psychosis. J Biol Chem 9 117. PMID: 26042007.

Kato et al (2015) Neurobehavioral Differences Between Mice Receiving Distinct Neuregulin Variants as Neonates; Impact on Sensitivity to MK-801. Cell Death Dis 15 222. PMID: 25817857.

Quillinan et al (2015) Region-specific role for GluN2B-containing NMDA receptors in injury to Purkinje cells and CA1 neurons following global cerebral ischemia. Neuropharmacology 284 555. PMID: 25450957.

Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Int J Neuropsychopharmacol 6 35458. PMID: 26461475.

Schitine et al (2015) Functional plasticity of GAT-3 in avian Müller cells is regulated by neurons via a glutamatergic input. PLoS One 82 42. PMID: 25700791.

Stephen et al (2015) Miro1 Regulates Activity-Driven Positioning of Mitochondria within Astrocytic Processes Apposed to Synapses to Regulate Intracellular Calcium Signaling. Front Behav Neurosci 35 15996. PMID: 26631479.

Velásquez-Martínez et al (2015) α-1 adrenoreceptors modulate GABA release onto ventral tegmental area dopamine neurons. BMC Neurosci 88 110. PMID: 25261018.

Wang et al (2015) MFN2 couples glutamate excitotoxicity and mitochondrial dysfunction in motor neurons. Nat Commun 290 168. PMID: 25416777.

Zhang et al (2015) Miro1 deficiency in amyotrophic lateral sclerosis. Cell Death Dis 7 100. PMID: 26074815.

Zou et al (2015) Oligodendrocytes Are Targets of HIV-1 Tat: NMDA and AMPA Receptor-Mediated Effects on Survival and Development. J Neurosci 35 11384. PMID: 26269645.

Deléglise et al (2014) β-amyloid induces a dying-back process and remote trans-synaptic alterations in a microfluidic-based reconstructed neuronal network. Acta Neuropathol Commun 2 145. PMID: 25253021.

Mirante et al (2014) Distinct molecular components for thalamic- and cortical-dependent plasticity in the lateral amygdala. J Neurosci 7 62. PMID: 25071439.

Pan et al (2014) Deranged NMDAergic cortico-subthalamic transmission underlies parkinsonian motor deficits. J Neuroinflammation 124 4629. PMID: 25202982.

Parnaudeau et al (2014) Glucocorticoid receptor gene inactivation in dopamine-innervated areas selectively decreases behavioral responses to amphetamine. Front Behav Neurosci 8 35. PMID: 24574986.

Sánchez-Blázquez et al (2014) The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Neurochem Int 17 1943. PMID: 24485144.

Lundgaard et al (2013) Neuregulin and BDNF induce a switch to NMDA receptor-dependent myelination by oligodendrocytes. PLoS Biol 11 e1001743. PMID: 24391468.

Tamburri et al (2013) NMDA-receptor activation but not ion flux is required for amyloid-β induced synaptic depression. PLoS One 8 e65350. PMID: 23750255.

Tsunekawa et al (2013) 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. J Neuroinflammation 14 4. PMID: 23289926.

Vicente-Sánchez et al (2013) HINT1 protein cooperates with cannabinoid 1 receptor to negatively regulate glutamate NMDA receptor activity. Mol Brain 6 42. PMID: 24093505.

Cassé et al (2012) Glutamate controls tPA recycling by astrocytes, which in turn influences glutamatergic signals. J Neurosci 32 5186. PMID: 22496564.

Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767. PMID: 22855824.

Kaufman et al (2012) Opposing roles of synaptic and extrasynaptic NMDA receptor signaling in cocultured striatal and cortical neurons. FASEB J 32 3992. PMID: 22442066.

Kocsis (2012) State-dependent increase of cortical gamma activity during REM sleep after selective blockade of NR2B subunit containing NMDA receptors. Sleep 35 1011. PMID: 22754048.

Lee and Sherman (2012) Intrinsic modulators of auditory thalamocortical transmission. Hear Res 287 43. PMID: 22726616.

Pedrazzi et al (2012) Potentiation of NMDA receptor-dependent cell responses by extracellular high mobility group box 1 protein. PLoS One 7 e44518. PMID: 22952988.

Rodríguez-Muñoz et al (2012) The mu-opioid receptor and the NMDA receptor associate in PAG neurons: implications in pain control. Neuropsychopharmacology 37 338. PMID: 21814188.

Straub et al (2011) Distinct functions of kainate receptors in the brain are determined by the auxiliary subunit Neto1. Nat Neurosci 14 866. PMID: 21623363.

Léveillé et al (2010) Suppression of the intrinsic apoptosis pathway by synaptic activity. J Neurosci 30 2623. PMID: 20164347.

Chao et al (2009) Na+ mechanism of delta-opioid receptor induced protection from anoxic K+ leakage in the cortex. Cell Mol Life Sci 66 1105. PMID: 19189047.

Gielen et al (2009) Mechanism of differential control of NMDA receptor activity by NR2 subunits. J Cereb Blood Flow Metab 459 703. PMID: 19404260.

Roselli et al (2009) Disassembly of shank and homer synaptic clusters is driven by soluble beta-amyloid(1-40) through divergent NMDAR-dependent signalling pathways. PLoS One 4 e6011. PMID: 19547699.

Furness et al (2008) 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). Neuroscience 157 80. PMID: 18805467.

Iwasato et al (2008) Cortical adenylyl cyclase 1 is required for thalamocortical synapse maturation and aspects of layer IV barrel development. J Neurosci 28 5931. PMID: 18524897.

Léveillé et al (2008) Neuronal viability is controlled by a functional relation between synaptic and extrasynaptic NMDA receptors. FASEB J 22 4258. PMID: 18711223.

Pais et al (2008) Necrotic neurons enhance microglial neurotoxicity through induction of glutaminase by a MyD88-dependent pathway. J Neurosci 5 43. PMID: 18844999.

Albright et al (2007) Increased thalamocortical synaptic response and decreased layer IV innervation in GAP-43 knockout mice. J Neurophysiol 98 1610. PMID: 17581849.

Steward et al (2007) A form of perforant path LTP can occur without ERK1/2 phosphorylation or immediate early gene induction. Learn Mem 14 433. PMID: 17562895.

Shin et al (2006) Vasoconstrictive neurovascular coupling during focal ischemic depolarizations. J Cereb Blood Flow Metab 26 1018. PMID: 16340958.

Calò et al (2005) Interactions between ephrin-B and metabotropic glutamate 1 receptors in brain tissue and cultured neurons. J Neurosci 25 2245. PMID: 15745950.

Shleper et al (2005) D-serine is the dominant endogenous coagonist for NMDA receptor neurotoxicity in organotypic hippocampal slices. Nature 25 9413. PMID: 16221850.

Liot et al (2004) 2,7-Bis-(4-amidinobenzylidene)-cycloheptan-1-one dihydrochloride, tPA stop, prevents tPA-enhanced excitotoxicity both in vitro and in vivo. Proc Natl Acad Sci U S A 24 1153. PMID: 15529015.

Tongiorgi et al (2004) Brain-derived neurotrophic factor mRNA and protein are targeted to discrete dendritic laminas by events that trigger epileptogenesis. J Neurosci 24 6842. PMID: 15282290.

Gabriel et al (2003) Transforming growth factor alpha-induced expression of type 1 plasminogen activator inhibitor in astrocytes rescues neurons from excitotoxicity. FASEB J 17 277. PMID: 12490542.

Valable et al (2003) Angiopoietin-1-induced PI3-kinase activation prevents neuronal apoptosis. Oncotarget 17 443. PMID: 12514118.

Rzeski et al (2001) Glutamate antagonists limit tumor growth. J Neurosci 98 6372. PMID: 11331750.

Matthies et al (2000) Enhancement of glutamate release by L-fucose changes effects of glutamate receptor antagonists on long-term potentiation in the rat hippocampus. Learn Mem 7 227. PMID: 10940323.

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