(+)-MK 801 Maleate

For research use only. Not for therapeutic Use.

  • CAT Number: I004841
  • CAS Number: 77086-22-7
  • Molecular Formula: C16H15N • C4H4O4
  • Molecular Weight: 337.40
  • Purity: ≥95%
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(+)-MK 801 Maleate(Cat No.: I004841), also known as Dizocilpine maleate, is a potent non-competitive antagonist of the N-methyl-D-aspartate (NMDA) receptor. It binds within the NMDA receptor channel, blocking calcium influx and inhibiting excitatory neurotransmission. Widely used in neuroscience research, (+)-MK 801 is valuable for studying excitotoxicity, neurodegenerative diseases, and schizophrenia models. Its effects on learning, memory, and synaptic plasticity provide insights into central nervous system function. The maleate salt enhances solubility for in vivo and in vitro experimental applications.


CAS Number 77086-22-7
Synonyms

(5S,10R)-5-methyl-10,11-dihydro-5H-5,10-epiminodibenzo[a,d][7]annulene maleate

Molecular Formula C16H15N • C4H4O4
Purity ≥95%
Target Membrane Transporter/Ion Channel
Solubility 10 mM in DMSO
Storage 3 years -20C powder
IC50 30.5 nM[1].
IUPAC Name (Z)-but-2-enedioic acid;(1S,9R)-1-methyl-16-azatetracyclo[7.6.1.02,7.010,15]hexadeca-2,4,6,10,12,14-hexaene
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
SMILES C[C@@]12C3=CC=CC=C3C[C@@H](N1)C4=CC=CC=C24.C(=C\C(=O)O)\C(=O)O
Reference

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<br>[1]. Wong EH, Kemp JA, Priestley T, The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proc Natl Acad Sci U S A. 1986 Sep;83(18):7104-8.
<br>[2]. Hirayama M, Kuriyama M. MK-801 is cytotoxic to microglia in vitro and its cytotoxicity is attenuated by glutamate, other excitotoxic agents and atropine. Possible presence of glutamate receptor and muscarinic receptor on microglia. Brain Res. 2001 Apr 6;897(1-2):204-6.
<br>[3]. van der Staay FJ, Rutten K, Erb C, Effects of the cognition impairer MK-801 on learning and memory in mice and rats. Behav Brain Res. 2011 Jun 20;220(1):215-29.
<br>[4]. Farley S, Dumas S, El Mestikawy S, Increased expression of the Vesicular Glutamate Transporter-1 (VGLUT1) in the prefrontal cortex correlates with differential vulnerability to chronic stress in various mouse strains: effects of fluoxetine and MK-801. Neuropharmacology. 2012 Jan;62(1):503-17.
<br>[5]. Kovacic P, Somanathan R. Clinical physiology and mechanism of dizocilpine (MK-801): electron transfer, radicals, redox metabolites and bioactivity. Oxid Med Cell Longev. 2010 Jan-Feb;3(1):13-22.
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