(+)-MK 801 maleate

(HB0004)

Product overview

  • Name
    (+)-MK 801 maleate
  • Short 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
  • Biological action
    Antagonist
  • Purity
    >98%
  • Our products in action

Images

Properties

  • Chemical name
    (5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate
  • Molecular Weight
    337.37
  • Chemical structure
    (+)-MK 801 maleate  [77086-22-7]
  • 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

Applications

  • 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.

     

     

Storing and Using Your Product

  • 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.

References for (+)-MK 801 maleate

  • Effects of MK-801 stereoisomers on schedule-controlled behavior in rats.

    Genovese RF et al (1991) Psychopharmacology (Berl) 105(4) : 477-80.
    PubMedID: 1771215
  • 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.
    PubMedID: 2154509
  • 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.
    PubMedID: 2821457
  • 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.
    PubMedID: 3529096
The following papers have cited the use of (+)-MK 801 maleate (HB0004) from Hello Bio. If you have published a paper using this product, and it is not shown here, then please tell us! We will send you a free gift as a thank you!
  • Desensitized D2 autoreceptors are resistant to trafficking.

    Robinson et al(2017) Sci Rep. 7(1) : 4379
    PubMedID: 28663556

Reviews

  • Verified customer, Research University Paris

    It does what it should! It is a very good product, delivered very rapidly.