ChemSpider 2D Image | (+)-Dizocilpine maleate | C20H19NO4

(+)-Dizocilpine maleate

  • Molecular FormulaC20H19NO4
  • Average mass337.369 Da
  • Monoisotopic mass337.131409 Da
  • ChemSpider ID4925623

  • Double-bond stereo - Double-bond stereo

    defined stereocentres - 2 of 2 defined stereocentres

More details:

Validated by Experts, Validated by Users, Non-Validated, Removed by Users

(+)-Dizocilpine maleate
(+)-10,11-dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-diyldiammonium maleate
(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine (Z)-2-Butenedioate (1:1)
(+)-MK 801 maleate
(+)-MK-801 (hydrogen maleate)
(+)-MK-801 hydrogen maleate
(1S,9R)-1-Methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaene (2Z)-2-butenedioate (1:1) [ACD/IUPAC Name]
(1S,9R)-1-Methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaene (2Z)-but-2-enedioate (1:1)
(2Z)-2-Butendisäure --(1S,9R)-1-methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaen (1:1) [German] [ACD/IUPAC Name]
(5S,10R)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate
More...

Validated by Experts, Validated by Users, Non-Validated, Removed by Users

MK 801 [DBID]
D03878 [DBID]
EU-0100872 [DBID]
M107_SIGMA [DBID]
MK-801 [DBID]
Prestwick_903 [DBID]
  • References
  • Experimental Physico-chemical Properties

    • Experimental Solubility:

      25 mM in water with gentle warming MedChem Express HY-15084
      Soluble in water (25mM, gentle warming) and in DMSO (100mM) Hello Bio HB0004
      Soluble to 25 mM in water and to 100 mM in DMSO Tocris Bioscience 0924, 924
  • Miscellaneous

    • Chemical Class:

      A maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid. ChEBI CHEBI:176788

    • Bio 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. Available as part of the Mixed NMDA Receptor Tocriset?. (-)-enantiomer also available. Tocris Bioscience 924
      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. Tocris Bioscience 924
      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. Tocris Bioscience 0924
      Biochemicals & small molecules/Antagonists & inhibitors Hello Bio HB0004
      Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM MedChem Express
      Dizocilpine maleate(MK 801) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM;IC50 Value: 30.5 nM[1].NMDA (N-methyl-D-aspartate) receptor antagonist (MK-801) were used to treat hyperalgesia in the diabetic neuropathic pain (DNP)[2].;In vitro: Neurophysiological studies in vitro, using a rat cortical-slice preparation, demonstrates a potent, selective, and noncompetitive antagonistic action of dizocilpine on depolarizing responses to N-Me-D-Asp but not to kainate or quisqualate. The potencies of phencyclidine, ketamine, SKF 10047, and the enantiomers of dizocilpine as N-Me-D-Asp antagonists correlate closely (r = 0.99) with their potencies as inhibitors of [3H] dizocilpine binding. This suggests that the dizocilpine binding sites are associated with N-Me-D-Asp receptors and provides an explanation for the mechanism of action of dizocilpine as an anticonvulsant[1]. The cytotoxicity of MK-801 on cultured microglia was also investigated. Cytotoxicity of MK MedChem Express HY-15084
      Glutamate (Ionotropic) Receptors Tocris Bioscience 924
      Ion Channels Tocris Bioscience 924
      Ion channels/Ligand-gated ion channel/Ionotropic glutamate receptors/NMDA Hello Bio HB0004
      Ligand-gated Ion Channels Tocris Bioscience 924
      Membrane Tranporter/Ion Channel; Neuronal Signaling; MedChem Express HY-15084
      NMDA Receptor MedChem Express HY-15084
      Non-competitive NMDA antagonist; acts at ion channel site Tocris Bioscience 0924, 924
      Potent, selective and non-competitive NMDA receptor antagonist (K<sub>d</sub> = 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. Hello Bio HB0004
      Potent, selective, non-competitive NMDA receptor antagonist Hello Bio HB0004

Predicted data is generated using the ACD/Labs Percepta Platform - PhysChem Module, version: 14.00

No predicted properties have been calculated for this compound.

Click to predict properties on the Chemicalize site


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