(+)-MK 801 maleate

(HB0004)
Technical documents: SDS CoA Datasheet

Product overview

Name (+)-MK 801 maleate
Description Potent, selective, non-competitive NMDA receptor antagonist
Biological description Potent, selective and non-competitive NMDA receptor antagonist (Kd = 37.2 nM). Approx 10-fold more potent than (-)-MK 801 maleate. Prevents calcium ion influx and long term potentiation induction. Shows anticonvulsant and neuroprotective properties.
Alternative names Dizocilpine maleate, Dizocilpine
Purity >98%
Customer comments

We are using MK801 in our research. We are very satisfied with the quality of this product. Verified customer, UCSD

(+)-MK 801 maleate does what it should! It is a very good product, delivered very rapidly. Verified customer, Research University Paris

...our first order with Hello Bio, has been satisfactory. The (+)-MK 801 Maleate has arrived in only some days and it was in perfect conditions. Verified customer, Universidad de La Laguna

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Biological Data

Application notes

The NMDA receptor antagonist (+)-MK 801 is use-dependent and blocks NMDARs in their open conformation.

(+)-MK 801 from Hello Bio fully abolishes evoked NMDAR currents at 10 μM rapidly upon repeated stimulations (see Fig 1 above). At concentrations of 50 μM a more rapid receptor blockade was observed.

 

#Protocol 1: Evoked NMDA receptor currents

  • Whole cell voltage clamp recordings were obtained from layer V neurons of the mouse prelimbic cortex brain slice.
  • NMDA currents were evoked via a stimulating electrode placed in layers II/III and evoked by a single square (150 μs) pulse every 10 sec at a stimulus intensity that gave a reliable NMDA current.
  • Neurons were held at +40 mV to relieve NMDA currents from their voltage-dependent Mg2+ block.
  • NMDA currents were continually stimulated and recorded in response to continual bath applications of (+)-MK 801 until NMDA currents were completely abolished.
  • All NMDAR recordings were made in the presence of GABAA-R and AMPAR antagonists.

 

 

Solubility & Handling

Storage instructions Room temperature
Solubility overview Soluble in water (25mM, gentle warming) and in DMSO (100mM)
Important This product is for RESEARCH USE ONLY and is not intended for therapeutic or diagnostic use. Not for human or veterinary use.

Calculators

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Dilution

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Chemical Data

Chemical name (5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate
Molecular Weight 337.37
Chemical structure Product image
Molecular Formula C16H15N.C4H4O4
CAS Number 77086-22-7
PubChem identifier 6420042
SMILES C[C@@]12C3=CC=CC=C3C[C@@H](N1)C4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
Source Synthetic
InChi InChI=1S/C16H15N.C4H4O4/c1-16-13-8-4-2-6-11(13)10-15(17-16)12-7-3-5-9-14(12)16;5-3(6)1-2-4(7)8/h2-9,15,17H,10H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t15-,16+;/m1./s1
InChiKey QLTXKCWMEZIHBJ-PJGJYSAQSA-N
MDL number MFCD00082465
Appearance White solid

References for (+)-MK 801 maleate

References are publications that support the biological activity of the product
  • Effects of MK-801 stereoisomers on schedule-controlled behavior in rats.

    Genovese RF et al (1991) Psychopharmacology (Berl) 105(4) : 477-80.
  • The effects of dizocilpine maleate (MK-801), an antagonist of the N-methyl-D-aspartate receptor, on neurologic recovery and histopathology following complete cerebral ischemia in primates.

    Lanier WL et al (1990) J Cereb Blood Flow Metab 10(2) : 252-61.
  • MK-801 blocks NMDA receptor-mediated synaptic transmission and long term potentiation in rat hippocampal slices.

    Coan EJ et al (1987) Neurosci Lett 80(1) : 111-4.
  • The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist.

    Wong EH et al (1986) Proc Natl Acad Sci U S A 83(18) : 7104-8.
Publications
These publications cite the use of (+)-MK 801 maleate purchased from Hello Bio:
  • Desensitized D2 autoreceptors are resistant to trafficking.

    Robinson et al (2017) Sci Rep. 7(1) : 4379
    PubMedID: 28663556
  • Differential Regulation of Evoked and Spontaneous Release by Presynaptic NMDA Receptors

    Abrahamsson et al (2017) Neuron 09 : 030
    PubMedID: 29033205
  • Cellular tolerance at the µ-opioid receptor is phosphorylation dependent

    Williams et al (2018) bioRxiv https://doi.org/ : 10.1101/252387
  • Synapse-specific Opioid Modulation of Thalamo-cortico-striatal Circuits

    Birdsong et al (2019) bioRxiv : https://doi.org/10.1101/525782
  • Phosphorylation-deficient G-protein-biased μ-opioid receptors improve analgesia and diminish tolerance but worsen opioid side effects.

    Kliewer et al (2019) Nat Commun 10(1) : 367
    PubMedID: 30664663

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