Dizocilpine (MK-801)

Dizocilpine is a non-competitive NMDA receptor antagonist.[1] It has potent anti-convulsant effects and probably dissociative anesthetic properties as well. However it is not used clinically for this purpose due to the discovery of Olney's lesions, a form of brain damage found to occur in rats. Although these probably do not occur in humans and other primates, it may still be too potent of an antagonist to have much clinical or recreational use.[2] Dizocilpine is commonly used in laboratory animals for experimental purposes. From recommendations of previous users, recreational doses range from under 1mg to 2mg orally, or 200-400µg taken intramuscularly.[3][4]

Dizocilpine molecule

In the 1980's, several clinical trials were conducted with dizocilpine on human patients. A study on adult ADD used doses up to 0.1-0.4mg a day, divided into three doses. Another study used doses of dizocilpine from 0.6-12mg a day in patients with Lennox-Gastaut syndrome. A high incidence of adverse experiences were reported including somnolence, ataxia, and mood changes.[5]

^ Fix AS, Horn JW, Wightman KA, et al. (1993). "Neuronal vacuolization and necrosis induced by the noncompetitive N-methyl-D-aspartate (NMDA) antagonist MK(+)801 (dizocilpine maleate): a light and electron microscopic evaluation of the rat retrosplenial cortex". Exp. Neurol. http://dx.doi.org/10.1006/exnr.1993.1153
^ Ontogeny of the N-Methyl-D-Aspartate (NMDA) Receptor System and Susceptibility to Neurotoxicity.
http://toxsci.oxfordjournals.org/cgi/content/full/68/1/9
^ Luke. "Disassociative Techniques & Castaneda". Erowid. http://www.erowid.org/experiences/exp.php?ID=46040
^ Tantric. "Experiences and Unguided Telepathy". Erowid. http://www.erowid.org/experiences/exp.php?ID=55729
^ Rogawski, M. A., & Porter, R. J. (1990). Antiepileptic drugs: pharmacological mechanisms and clinical efficacy with consideration of promising developmental stage compounds. Pharmacological Reviews, 42(3).

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