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About: Dizocilpine     Goto   Sponge   NotDistinct   Permalink

An Entity of Type : umbel-rc:DrugProduct, within Data Space : dbpedia.demo.openlinksw.com associated with source document(s)

Type: Thingdul:ChemicalObjectchemical substanceDrugyago:WikicatMolecularFormulasyago:Abstraction100002137yago:Agent114778436yago:CausalAgent100007347yago:Communication100033020yago:DesignerDrug103179489yago:Drug103247620yago:Formula106816935yago:Matter100020827yago:Message106598915yago:MolecularFormula106817173yago:PhysicalEntity100001930yago:PsychoactiveDrug104017137drugyago:Statement106722453yago:Substance100020090yago:WikicatDesignerDrugsyago:WikicatDissociativeDrugsumbel-rc:DrugProduct New Facet based on Instances of this Class

Dizocilpine (INN), also known as MK-801, is a pore blocker of the N-Methyl-D-aspartate (NMDA) receptor, a glutamate receptor, discovered by a team at Merck in 1982. Glutamate is the brain's primary excitatory neurotransmitter. The channel is normally blocked with a magnesium ion and requires depolarization of the neuron to remove the magnesium and allow the glutamate to open the channel, causing an influx of calcium, which then leads to subsequent depolarization. Dizocilpine binds inside the ion channel of the receptor at several of PCP's binding sites thus preventing the flow of ions, including 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 acts as a potent