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- Dizocilpine abstract "Dizocilpine (INN), also known as MK-801, is a non-competitive antagonist 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. MK-801 binds inside the ion channel of the receptor at several of PCP's binding sites thus preventing the flow of ions, including an influx of 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 anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions (see below), in test rats. MK-801 is also associated with a number of negative side effects, including cognitive disruption and psychotic-spectrum reactions. It also inhibited the induction of long term potentiation. Instead, the NMDA receptor pore-blocker ketamine is used as a dissociative anesthetic in human medical procedures. While ketamine may also trigger temporary psychosis in certain individuals, its short half-life and lower potency make it a much safer clinical option. However, dizocilpine is the most frequently used non-competitive NMDA receptor antagonist in animal models to mimic psychosis for experimental purposes.Dizocilpine has also been found to act as a nicotinic acetylcholine receptor antagonist. It has been shown to bind to and inhibit the serotonin and dopamine transporters as well.".
- Dizocilpine atcPrefix "?".
- Dizocilpine atcSuffix "?".
- Dizocilpine casNumber "77086-21-6".
- Dizocilpine drugbank "?".
- Dizocilpine fdaUniiCode "7PY8KH681I".
- Dizocilpine iupacName "[5R,10S]-[+]-5-methyl-10,11- dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine".
- Dizocilpine pubchem "180081".
- Dizocilpine thumbnail Dizocilpine.svg?width=300.
- Dizocilpine wikiPageExternalLink pmidlookup?view=long&pmid=3529096.
- Dizocilpine wikiPageExternalLink exp_Dizocilpine.shtml.
- Dizocilpine wikiPageID "1194091".
- Dizocilpine wikiPageRevisionID "597182964".
- Dizocilpine atcPrefix "?".
- Dizocilpine atcSuffix "?".
- Dizocilpine bioavailability "?".
- Dizocilpine c "16".
- Dizocilpine casNumber "77086".
- Dizocilpine chembl "284237".
- Dizocilpine chemspiderid "156718".
- Dizocilpine drugbank "?".
- Dizocilpine eliminationHalfLife "?".
- Dizocilpine excretion "?".
- Dizocilpine h "15".
- Dizocilpine hasPhotoCollection Dizocilpine.
- Dizocilpine inchi "1".
- Dizocilpine inchikey "LBOJYSIDWZQNJS-CVEARBPZBY".
- Dizocilpine iupacName "[5R,10S]-[+]-5-methyl-10,11- dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine".
- Dizocilpine iupharLigand "2403".
- Dizocilpine meltingPoint "68.75".
- Dizocilpine metabolism "?".
- Dizocilpine molecularWeight "221.297".
- Dizocilpine n "1".
- Dizocilpine pregnancyAu "?".
- Dizocilpine pregnancyUs "/".
- Dizocilpine pubchem "180081".
- Dizocilpine routesOfAdministration "Oral, IM".
- Dizocilpine smiles "C[C@]1C4=C3C=CC=C4".
- Dizocilpine stdinchi "1".
- Dizocilpine stdinchikey "LBOJYSIDWZQNJS-CVEARBPZSA-N".
- Dizocilpine unii "7".
- Dizocilpine verifiedfields "changed".
- Dizocilpine verifiedrevid "460959675".
- Dizocilpine watchedfields "changed".
- Dizocilpine subject Category:Designer_drugs.
- Dizocilpine subject Category:Dibenzocycloheptenes.
- Dizocilpine subject Category:Dissociative_drugs.
- Dizocilpine subject Category:NMDA_receptor_antagonists.
- Dizocilpine type Adversary109773245.
- Dizocilpine type CausalAgent100007347.
- Dizocilpine type LivingThing100004258.
- Dizocilpine type NMDAReceptorAntagonists.
- Dizocilpine type Object100002684.
- Dizocilpine type Organism100004475.
- Dizocilpine type Person100007846.
- Dizocilpine type PhysicalEntity100001930.
- Dizocilpine type Whole100003553.
- Dizocilpine type YagoLegalActor.
- Dizocilpine type YagoLegalActorGeo.
- Dizocilpine type Drug.
- Dizocilpine type DrugProduct.
- Dizocilpine type FunctionalSubstance.
- Dizocilpine comment "Dizocilpine (INN), also known as MK-801, is a non-competitive antagonist 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 label "Dizocilpine".
- Dizocilpine label "Dizocylpina".
- Dizocilpine label "MK-801".
- Dizocilpine sameAs MK-801.
- Dizocilpine sameAs Dizocylpina.
- Dizocilpine sameAs m.04g74w.
- Dizocilpine sameAs Q4386371.
- Dizocilpine sameAs Q4386371.
- Dizocilpine sameAs Dizocilpine.
- Dizocilpine wasDerivedFrom Dizocilpine?oldid=597182964.
- Dizocilpine depiction Dizocilpine.svg.
- Dizocilpine isPrimaryTopicOf Dizocilpine.
