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MK-801

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Subjective Effects
Interactions
Tolerance
Legality
MK-801 molecule structureMK-801 molecule structure
Dizocilpine
Open in Piru
Psychoactive Class
DissociativeHallucinogen

MK-801 is a dissociative research chemical reported to resemble PCP and ketamine in its effects. It is classified as habit-forming.

Dosage & Duration

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Dosage

Doses are population estimates that vary widely between individuals.

Moderate50-100 µg

Duration

After Effects1-72 hours
Total20-36 hours

Subjective Effects

Subjective Effects not written up yet

Pharmacology

Pharmacodynamics

MK-801 blocks the NMDA receptor pore, binding within the open ion channel at PCP binding sites and preventing ion flow, including calcium entry. This uncompetitive blockade depends on channel use and membrane voltage.1 In experimental seizure models, MK-801 showed anticonvulsant activity,2 preventing the development of kindled seizures without affecting established kindled seizures. Secondary actions include antagonism of nicotinic acetylcholine receptors3 and inhibition of serotonin and dopamine transporters.

MK-801 has demonstrated neuroprotective effects in cell cultures and animal models of excitotoxic injury. It also reduced rabies virus production approximately 1,000-fold in infected rat cortical neurons through an unknown mechanism, without directly inactivating the virus in a cell-free suspension.

Pharmacokinetics

Absorption & half-lifenot documented yetMetabolitesnone documented yet

Interactions

Interactions not written up yet

An unlisted combination is an unknown one, not a safe one. Check a dedicated combination chart before mixing.

Check TripSit

Tolerance

Tolerance not written up yet

Harm Potential

Addiction & Dependence

Psychological

MK-801 has reinforcing and habit-forming potential: rats self-administered injections into the nucleus accumbens and frontal cortex, intraperitoneal administration increased self-stimulation responding, and animals developed conditioned place preference; its rewarding effect was not dependent on dopamine. In rhesus monkeys previously trained to self-administer other drugs, three of four trained with phencyclidine self-administered MK-801,5 whereas none of four trained with cocaine did.

Toxicity

Brain

MK-801 caused neuronal vacuolization and necrosis in the posterior cingulate/retrosplenial cortex of laboratory rats;6 vacuoles began forming within 30 minutes after a subcutaneous dose of 1 mg/kg.7 It also impaired acquisition of difficult, but not easy, learning tasks in rats and primates.

Psychosis Risk

MK-801 is associated with psychotic-spectrum reactions and is particularly prone to producing psychotomimetic effects, including hallucinations, through NMDA receptor blockade. In laboratory animals, a single injection reproduced positive and negative schizophrenia-like symptoms; repeated higher-dose administration also reproduced neurochemical alterations resembling those found in first-episode schizophrenia.

History & Culture

Dizocilpine, also known as MK-801, was discovered by a team at Merck in 1982. Merck pursued its development as a potential neuroprotective agent but later discontinued the program.9…

Legality

Legality not written up yet

References

Source Pages

  1. Bluelight: MK-801 (4 mg sublingual) trip report
  2. Bluelight: MK-801 2.5 mg total (IM + rectal) trip report
  3. Erowid Experience: 3mg oral trip report
  4. Erowid Experience: IM dosing series
  5. Erowid Experience: The Most Beautiful Lobotomy I Ever Had
  6. TripSit: MK-801 Factsheet
  7. Wikipedia
  8. Wikipedia: Olney's lesions

Citations

  1. Block of N-methyl-D-aspartate-activated current by the anticonvulsant MK-801: selective binding to open channels. PubMed / Proceedings of the National Academy of Sciences (1988). https://doi.org/10.1073/pnas.85.4.13071
  2. Anticonvulsant and antiepileptogenic actions of MK-801 in the kindling and electroshock models.. Scholars@Duke / Neuropharmacology (1988). https://doi.org/10.1016/0028-3908(88)90176-11
  3. The anticonvulsant MK-801 interacts with peripheral and central nicotinic acetylcholine receptor ion channels. PubMed / The Journal of Pharmacology and Experimental Therapeutics (1990). https://pubmed.ncbi.nlm.nih.gov/169489512
  4. Pharmacological Comparative Characterization of REL-1017 (Esmethadone-HCl) and Other NMDAR Channel Blockers in Human Heterodimeric N-Methyl-D-Aspartate Receptors. MDPI / Pharmaceuticals (2022). https://doi.org/10.3390/ph150809971
  5. The self-administration of MK-801 can depend upon drug-reinforcement history, and its discriminative stimulus properties are phencyclidine-like in rhesus monkeys. Journal of Pharmacology and Experimental Therapeutics (1990). https://pubmed.ncbi.nlm.nih.gov/21811131
  6. Pathomorphologic effects of N-methyl-D-aspartate antagonists in the rat posterior ingulate/retrosplenial cerebral cortex: A review. Drug Development Research (1994). https://doi.org/10.1002/ddr.43032030412
  7. Neuronal vacuole formation in the rat posterior cingulate/retrosplenial cortex after treatment with the N-methyl-d-aspartate (NMDA) antagonist MK-801 (dizocilpine maleate). Acta Neuropathologica (1994). https://doi.org/10.1007/bf002964871
  8. The drug MK-801 attenuates the development, but not the expression, of long-term potentiation and stimulus train-induced bursting in hippocampal slices. Neuropharmacology (1989). https://doi.org/10.1016/0028-3908(89)90076-21
  9. An Oral History of Neuropsychopharmacology: The First Fifty Years, Volume 3: Neuropharmacology. American College of Neuropsychopharmacology (2011). https://acnp.org/wp-content/uploads/2017/10/Volume3.pdf1
  10. Behavioral features and disorganization of oscillatory activity in C57BL/6J mice after acute low dose MK-801 administration. Frontiers in Neuroscience (2022). https://doi.org/10.3389/fnins.2022.10018691

Further Reading

  1. Clinical physiology and mechanism of dizocilpine (PMC)
  2. Multiple-drug fatality case (MK-801 + benzodiazepines + alcohol)
  3. Plasma and brain half-life in rats (PubMed)
  4. Lladó-Pelfort et al. 2017 - Effects of Hallucinogens on Neuronal Activity

Article Status

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