Dizocilpine

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Dizocilpine
Systematic (IUPAC) name
(+)-5-methyl-10,11- dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine maleate)
Identifiers
CAS number	77086-21-6
ATC code	??
PubChem	1207
DrugBank	?
Chemical data
Formula	C₁₆H₁₅N
Mol. weight	221.297
Physical data
Melt. point	68.75 °C (156 °F)
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?(AU) ?(US)
Legal status	?(AU)
Routes	Oral, IM

Dizocilpine, also known as MK-801, is a non-competitive NMDA receptor antagonist. It binds inside the ion channel of the receptor and thus prevents the flow of calcium ions through the channel. 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 is an anti-convulsant.

1 Possible future medical uses
2 Recreational use
3 References
4 External links

[edit] Possible future medical uses

The effects of MK-801 at NMDA receptors are clear and significant. Since NMDA receptors are key in the progression of excitotoxicity, NMDA receptor antagonists including MK-801 have been extensively studied for use in treatment of diseases with excitotoxic components, such as stroke, traumatic brain injury, and neurodegenerative diseases such as Huntington's, Alzheimer's, and amyotrophic lateral sclerosis. MK-801 has shown effectiveness protecting neurons in cell culture and animal models of excitotoxic neurodegeneration (Ayala and Tapia, 2005; Kocaeli et al., 2005; Mukhin et al., 1997). However, NMDA antagonists like MK-801 have largely failed to show safety and effectiveness in clinical trials, possibly due to inhibition of NMDA receptor function that is necessary for normal neuronal function. Since MK-801 is a particularly strong NMDA receptor antagonist, this drug is particularly likely to have psychotomimetic side effects (such as hallucinations) that result from NMDA receptor blockade. MK-801 had a promising future as a neuroprotective agent until neurotoxic-like effects were seen in certain brain regions. Merck, a drug company, promptly dropped development of MK-801.

[edit] Recreational use

MK-801 is effective as a recreational drug active in the 50-100μg range. Some users report that the experience is not pleasant; it is often accompanied by strong aural hallucinations.