(+)MK-801 maleate is an uncompetitive antagonist of the N-Methyl-D-aspartate (NMDA) receptor. Dizocilpine blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. The drug acts as a potent anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions (see below), in test rats. Dizocilpine is the most frequently used non-competitive NMDA receptor antagonist in animal models to mimic psychosis for experimental purposes.
Chemical Formula: C20H19NO4
Molecular Weight: 337.375
Elemental Analysis: C, 71.20; H, 5.68; N, 4.15; O, 18.97
InChi Code: 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-
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
[3H]Dizocilpine maleate binds with NMDA receptor with a Kd of 37.2±2.7 nM in rat cerebral cortical membranes.
Dizocilpine maleate causes a progressive, long-lasting blockade of current induced by N-Me-D-Asp.
Dizocilpine maleate progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine (MK-801) is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches.
Dizocilpine maleate (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (MK-801; <500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.
Dizocilpine maleate (MK 801 maleate) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.
Dizocilpine maleate (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine maleate (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
Dizocilpine maleate (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg.
Abuhamdah RM, Hussain MD, Chazot PL, Ennaceur A. Pre-training in a radial arm maze abolished anxiety and impaired habituation in C57BL6/J mice treated with dizocilpine. Physiol Behav. 2016 Jun 15. pii: S0031-9384(16)30416-4. doi: 10.1016/j.physbeh.2016.06.017. [Epub ahead of print] PubMed PMID: 27317838.
Vojtechova I, Petrasek T, Hatalova H, Pistikova A, Vales K, Stuchlik A. Dizocilpine (MK-801) impairs learning in the active place avoidance task but has no effect on the performance during task/context alternation. Behav Brain Res. 2016 May 15;305:247-57. doi: 10.1016/j.bbr.2016.03.020. Epub 2016 Mar 10. PubMed PMID: 26970577.
Gao ZY, Yang P, Huang QJ, Xu HY. The influence of dizocilpine on the reserpine-induced behavioral and neurobiological changes in rats. Neurosci Lett. 2016 Feb 12;614:89-94. doi: 10.1016/j.neulet.2016.01.006. Epub 2016 Jan 11. PubMed PMID: 26779676.
Khan N, Saad A, Nurulain SM, Darras FH, Decker M, Sadek B. The dual-acting H3 receptor antagonist and AChE inhibitor UW-MD-71 dose-dependently enhances memory retrieval and reverses dizocilpine-induced memory impairment in rats. Behav Brain Res. 2016 Jan 15;297:155-64. doi: 10.1016/j.bbr.2015.10.022. Epub 2015 Oct 20. PubMed PMID: 26467607.
Bloch K, Gil-Ad I, Tarasenko I, Vanichkin A, Taler M, Hornfeld SH, Vardi P, Weizman A. Intracranial pancreatic islet transplantation increases islet hormone expression in the rat brain and attenuates behavioral dysfunctions induced by MK-801 (dizocilpine). Horm Behav. 2015 Jun;72:1-11. doi: 10.1016/j.yhbeh.2015.04.019. Epub 2015 May 2. PubMed PMID: 25943974.
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