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Chemical Structure| 77086-22-7 Chemical Structure| 77086-22-7

Structure of Dizocilpine maleate
CAS No.: 77086-22-7

Chemical Structure| 77086-22-7

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Dizocilpine maleate (MK-801 maleate) is a potent, selective, and non-competitive NMDA receptor antagonist with a Kd of 37.2 nM in rat brain membranes.

Synonyms: MK-801 maleate; (+)-MK-801(hydrogen maleate); Dizocilpine

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Product Details of Dizocilpine maleate

CAS No. :77086-22-7
Formula : C20H19NO4
M.W : 337.37
SMILES Code : C[C@]1(N2)C3=CC=CC=C3C[C@]2([H])C4=CC=CC=C14.O=C(O)/C=C\C(O)=O
Synonyms :
MK-801 maleate; (+)-MK-801(hydrogen maleate); Dizocilpine
MDL No. :MFCD00082465
InChI Key :QLTXKCWMEZIHBJ-PJGJYSAQSA-N
Pubchem ID :6420042

Safety of Dizocilpine maleate

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P280-P305+P351+P338

Isoform Comparison

Biological Activity

Target
  • NMDA receptor

    NMDA receptor, Kd:37.2 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
SH-SY5Y cells 0.3 to 10 µM 24 hours To assess the cytotoxicity of Dizocilpine maleate, results showed that Dizocilpine maleate did not significantly reduce cell viability at concentrations ranging from 0.3 to 10 µM. PMC1876571
mouse cortical slices 100 μM and above Dizocilpine significantly inhibited veratridine- and potassium-stimulated release of glutamate and aspartate at concentrations of 100 μM and above. PMC1909187
Primary cortical neurons 20μM 72 hours To investigate the effect of MK-801 on the expression of Pdlim5 and CRTC1 in neurons, results showed that MK-801 increased Pdlim5 and p-CRTC1 levels and decreased CRTC1 expression. PMC10042998

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice DBA/2 mouse model Intravenous injection 40 mg/kg Daily for 15 days To evaluate the effect of Dizocilpine maleate on improving sensory gating deficits, results showed that Dizocilpine maleate significantly improved sensory gating deficits at doses of 0.3 and 1 mg/kg. PMC1876571
Mice C57BL6J and GIN mice Perfusion 300 mg/kg and 1200 mg/kg Daily for 2 or 3 months MK-801 completely inhibited CSD initiation, eliminating the third depolarization peak and the steep IOS rise. PMC10408042
Mice MK-801-induced schizophrenia-like behavior model Intraperitoneal injection 1200 ppm Up to 6 months To investigate the effect of MK-801 on schizophrenia-like behavior and cognitive deficits in mice, results showed that MK-801 significantly decreased mouse performance in the PPI task and impaired mouse WM, indicating it induced schizophrenia-like behavior and cognitive deficits. PMC10042998
Mice Cognitive impairment model Intraperitoneal injection 0.2 mg/kg Single injection Establish a cognitive impairment model to evaluate the effects of Dizocilpine maleate on cognitive behavior in mice. PMC7520443

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.96mL

0.59mL

0.30mL

14.82mL

2.96mL

1.48mL

29.64mL

5.93mL

2.96mL

References

 

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