Dizocilpine



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
N 
Mol. mass 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
Routes Oral, IM

Dizocilpine, also known as MK-801, is a non-competitive calcium (Ca2+) 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.

Possible future medical uses

The effects of MK-801 at NMDA receptors are clear and significant. NMDA receptors are key in the progression of Merck, a drug company, promptly dropped development of MK-801.

Recreational use

Dizocilpine may be effective as a recreational drug, and may have an active dose in the 50-100μg range. Little is known in this context about its effects, dosage, and risks. Dizocilpine's high potency makes its dosage more difficult to accurately control when compared to other similar drugs. As a result, the chances of phencyclidine (PCP), and causes far worse amnesia and residual deficits in thinking, which have hindered its acceptance as a recreational drug.[citation needed]

References

  1. ^ Ayala GX, Tapia R. 2005. Late N-methyl-D-aspartate receptor blockade rescues hippocampal neurons from excitotoxic stress and death after 4-aminopyridine-induced epilepsy. European Journal of Neuroscience. Volume 22, Issue 12, Pages 3067-3076. Accessed January 7, 2007.
  2. ^ Kocaeli H, Korfali E, Ozturk H, Kahveci N, Yilmazlar S. 2005. MK-801 improves neurological and histological outcomes after spinal cord ischemia induced by transient aortic cross-clipping in rats. Surgical Neurology. Volume 64, Supplement 2, Pages S22-S26; discussion S27. Accessed January 7, 2007.
  3. ^ Mukhin AG, Ivanova SA, Knoblach SM and Faden AI. 1997. New in vitro model of traumatic neuronal injury: Evaluation of secondary injury and glutamate receptor-mediated neurotoxicity. Journal of Neurotrauma. Volume 14, Issue 9, Pages 651-663. Accessed January 7, 2007.
  4. ^ Olney J, Labruyerre J and Price MT. 1989. Pathological changes induced in cerebrocortical neurons by phencyclidine and related drugs. Science, Volume 244, Issue 4910, Pages 1360-1362. Accessed January 7, 2007.
  5. ^ Ellison G. 1995. The N-methyl-D-aspartate antagonists phencyclidine, ketamine and dizocilpine as both behavioral and anatomical models of the dementias. Brain Research. Brain Research Reviews, Volume 20, Issue 2, Pages 250-267. Accessed January 7, 2007.


 
This article is licensed under the GNU Free Documentation License. It uses material from the Wikipedia article "Dizocilpine". A list of authors is available in Wikipedia.