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Submit Review(+)-MK 801 maleate
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% (HPLC)
Biological Activity for (+)-MK 801 maleate
(+)-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.
Compound Libraries for (+)-MK 801 maleate
(+)-MK 801 maleate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for (+)-MK 801 maleate
| M. Wt | 337.37 |
| Formula | C16H15N.C4H4O4 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 77086-22-7 |
| PubChem ID | 6420042 |
| InChI Key | QLTXKCWMEZIHBJ-PJGJYSAQSA-N |
| Smiles | O=C(O)/C=C\C(O)=O.C[C@]1(N4)C3=C(C=CC=C3)C[C@@H]4C2=C1C=CC=C2 |
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.
Solubility Data for (+)-MK 801 maleate
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 3.37 | 10 with gentle warming | |
| DMSO | 33.74 | 100 |
Preparing Stock Solutions for (+)-MK 801 maleate
The following data is based on the product molecular weight 337.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.96 mL | 14.82 mL | 29.64 mL |
| 5 mM | 0.59 mL | 2.96 mL | 5.93 mL |
| 10 mM | 0.3 mL | 1.48 mL | 2.96 mL |
| 50 mM | 0.06 mL | 0.3 mL | 0.59 mL |
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Product Datasheets for (+)-MK 801 maleate
References for (+)-MK 801 maleate
References are publications that support the biological activity of the product.
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
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
Wong et al (1986) The anticonvulsant MK 801 is a potent N-MthD.-aspartate antagonist. Proc.Natl.Acad.Sci.U.S.A. 83 7104 PMID: 3529096
Zajaczkowski et al (1997) Uncompetitive NMDA receptor antagonists attenuate NMDA-induced impairment of passive avoidance learning and LTP. Neuropharmacology 36 961 PMID: 9257940
Carey et al (1998) Effects of dizocilpine (MK-801) on motor activity and memory. Psychopharmacology 137 241 PMID: 9683001
Ding et al (2018) Effect of NMDA on proliferation and apoptosis in hippocampal neural stem cells treated with MK-801. Exp.Ther.Med. 16 1137 PMID: 30116364
If you know of a relevant reference for (+)-MK 801 maleate, please let us know.
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Keywords: (+)-MK 801 maleate, (+)-MK 801 maleate supplier, Non-competitive, NMDA, antagonists, ion, channel, site, Glutamate, Receptors, N-Methyl-D-Aspartate, iGlur, Ionotropic, (+)-MK801, maleate, MK801, apoptotic, apoptosis, antiproliferative, Dizocilpine, 0924, Tocris Bioscience
91 Citations for (+)-MK 801 maleate
Citations are publications that use Tocris products. Selected citations for (+)-MK 801 maleate include:
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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
Cipriani et al (2015) FTY720 attenuates excitotoxicity and neuroinflammation. Curr Mol Med 12 86 PMID: 25953296
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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
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Baxter et al (2015) Synaptic NMDA receptor activity is coupled to the transcriptional control of the glutathione system. Neuroscience 6 6761 PMID: 25854456
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
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O'Donnell et al (2016) Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes. J Neurosci 36 7109 PMID: 27383588
Gaamouch et al (2012) Interaction between αCaMKII and GluN2B controls ERK-dependent plasticity. J Neurosci 32 10767 PMID: 22855824
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Léveillé et al (2010) Suppression of the intrinsic apoptosis pathway by synaptic activity. J Neurosci 30 2623 PMID: 20164347
González-Rueda et al (2018) Activity-Dependent Downscaling of Subthreshold Synaptic Inputs during Slow-Wave-Sleep-like Activity In Vivo. Neuron 97 1244 PMID: 29503184
Sánchez-Blázquez et al (2018) Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice. Int J Neuropsychopharmacol 21 938 PMID: 29860313
McKay et al (2018) The Developmental Shift of NMDA Receptor Composition Proceeds Independently of GluN2 Subunit-Specific GluN2 C-Terminal Sequences. Cell Rep 25 841 PMID: 30355491
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Marinangeli et al (2018) AMP-Activated Protein Kinase Is Essential for the Maintenance of Energy Levels during Synaptic Activation. iScience 9 1 PMID: 30368077
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Product performed ideally over years and would buy again..
By
Anonymous on 04/04/2020
Assay Type: In Vitro
Species: Rat
Cell Line/Tissue: Sprague-Dawley rats primary neuronal
10 μM MK-801 for 10 min
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