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 acts as an NMDA receptor antagonist. It is selective and potent, but noncompetitive, used in various ischemia treatments.
Uses
(-)-MK-801 MALEATE is probe for NMDA receptors
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 Ca
2+ 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 Ca
2+ 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
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.
