神经信号
CAS号：77086-21-6
品名：5H-Dibenzo[a,d]cyclohepten-5,10-imine,10,11-dihydro-5-methyl-,(5S,10R)-
中文别名：地佐环平;
英文别名：Dizocilpine;
分子式：C16H15N
分子量：221.297
精确质量：221.12
Psa：12.03
密度：
海关编码：2925290090
简介：Dizocilpine(INN),alsoknownasMK-801,isanuncompetitiveantagonistoftheN-Methyl-D-aspartate(NMDA)receptor,aglutamatereceptor,discoveredbyateamatMerckin1982.Glutamateisthebrain'sprimaryexcitatoryneurotransmitter.Thechannelisnormallyblockedwithamagnesiumionandrequiresdepolarizationoftheneurontoremovethemagnesiumandallowtheglutamatetoopenthechannel,causinganinfluxofcalcium,whichthenleadstosubsequentdepolarization.DizocilpinebindsinsidetheionchannelofthereceptoratseveralofPCP'sbindingsitesthuspreventingtheflowofions,includinganinfluxofcalcium(Ca2+),throughthechannel.DizocilpineblocksNMDAreceptorsinause-andvoltage-dependentmanner,sincethechannelmustopenforthedrugtobindinsideit.Thedrugactsasapotentanti-convulsantandlikelyhasdissociativeanestheticproperties,butitisnotusedclinicallyforthispurposeduetothediscoveryofbrainlesions,calledOlney'slesions(seebelow),intestrats.Dizocilpineisalsoassociatedwithanumberofnegativesideeffects,includingcognitivedisruptionandpsychotic-spectrumreactions.Italsoinhibitedtheinductionoflongtermpotentiation.Instead,theNMDAreceptorpore-blockerketamineisusedasadissociativeanestheticinhumanmedicalprocedures.Whileketaminemayalsotriggertemporarypsychosisincertainindividuals,itsshorthalf-lifeandlowerpotencymakeitamuchsaferclinicaloption.However,dizocilpineisthemostfrequentlyusednon-competitiveNMDAreceptorantagonistinanimalmodelstomimicpsychosisforexperimentalpurposes.
