(+)-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 / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

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:

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

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.

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.

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

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.

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.

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.

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

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.

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.

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.

Do you know of a great paper that uses (+)-MK 801 maleate from Tocris? If so please let us know.show all ▼show less ▲

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