For research use only. Not Intended for Therapeutic Use!
|Molecular Formula:||C16H15N • C4H4O4|
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|Product-Name:||(+)-MK 801 Maleate|
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.
NMDA (N-methyl-D-aspartate) receptor antagonist (MK-801) were used to treat hyperalgesia in the diabetic neuropathic pain (DNP).
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. The cytotoxicity of MK-801 on cultured microglia was also investigated. Cytotoxicity of MK-801 was reduced by the addition of L-glutamate, kainate and NMDA. The action of MK-801 was due to the direct action of microglia.
in vivo: MK-801, administered s.c. or i.p. into rodents in doses up to 0.1 mg kg(-1), appears to fulfill the criteria of our definition of a cognition impairer in rodents, without causing sensorimotor impairments and/or signs of intoxication. In addition, MK-801-treated rodents appear to fulfill the criteria of a valid animal model of cognitive dysfunctions, with robust effects across species, housing conditions, and testing paradigms. Administration of an antagonist of NMDA receptors, MK-801, induced antidepressant-like effects in the TST for stressed BALB/c, but was ineffective for the hyperactivity and anhedonia-like behavior, in contrast to fluoxetine. Chronic MK-801 was totally inactive on the behavior of stressed C57BL/6 mice. MK-801, but not fluoxetine, inhibited the VGLUT1 prefrontal increase in BALB/c.
Clinical trial: Clinical physiology and mechanism of dizocilpine (MK-801) was reported in 2010.
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. 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.
. 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.
. 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.
. 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.