(-)-MK-801 MALEATE Property

Melting point:

208.5-210°

alpha 

D20 +114° (c = 0.0128 g/2 ml ethanol)

storage temp. 

Inert atmosphere,2-8°C

solubility 

DMSO: >20 mg/mL

form 

solid

color 

white

optical activity

[α]25/D +117°, c = 1 in methanol(lit.)

InChIKey

QLTXKCWMEZIHBJ-FWHYOZOBSA-N

Safety

Safety Statements 

22-24/25

WGK Germany 

3

RTECS 

HP1093575

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

H319Causes serious eye irritation

H361Suspected of damaging fertility or the unborn child

H370Causes damage to organs

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P281Use personal protective equipment as required.

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P307+P311IF exposed: call a POISON CENTER or doctor/physician.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P321Specific treatment (see … on this label).

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

(-)-MK-801 MALEATE Chemical Properties,Usage,Production

Uses

Dizocilpine maleate is used to interact at the NMDA-associated ion channel, preventing Ca2+ flux and blocking NMDA-induced depolarizations. (+)-MK 801 demonstrates potent neuroprotective effects against excitotoxic insult, showing substantial protection against neuron loss produced by NMDA and quinolinic acid introduction.

Uses

(-)-MK-801 MALEATE is probe for NMDA receptors

Uses

(-)-MK-801 MALEATE acts as an NMDA receptor antagonist. It is selective and potent, but noncompetitive, used in various ischemia treatments.

Definition

ChEBI: Dizocilpine maleate is a maleate salt obtained by reaction of dizocilpine with one equivalent of maleic acid. It has a role as an anaesthetic, an anticonvulsant, a neuroprotective agent, a nicotinic antagonist and a NMDA receptor antagonist. It is a maleate salt and a tetracyclic antidepressant. It contains a dizocilpine(1+).

General Description

A highly potent, selective and non-competitive NMDA receptor antagonist that acts by binding to a site located within the NMDA associated ion channel, preventing Ca²⁺ flux. An effective anti-ischemic agent in several animal models. Has been used to develop an in vivo model of NMDA receptor-dependent apoptotic neurodegenerative disease in developing rat brains. Has also been used to develop an in vitro model of NMDA receptor-specific Ca²⁺ entry induced seizures.

Biological Activity

(-)-MK-801 MALEATE is 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 Ca 2+ flux. An effective anti-ischemic agent in several animal models. Also available as part of the Mixed NMDA Receptor Tocriset™ .

Biochem/physiol Actions

Primary TargetNMDA receptor

storage

Room temperature

References

[1] wong eh, kemp ja, priestley t, knight ar, woodruff gn, iversen ll . 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.