代谢

CAS号：1292799-56-4

品名：苏木精Quinoline,2-​[[4-​[1-​(methyl-​11C)​-​4-​(4-​pyridinyl)​-​1H-​pyrazol-​3-​yl]​phenoxy]​methyl]​-

中文别名：苏木精

英文别名：2-((4-(1-methyl-4-(pyridin-4-yl)-1H-pyrazol-3-yl)phenoxy)methyl)quinoline;2-((4-(1-(methyl-11c)-4-(4-pyridinyl)-1h-pyrazol-3-yl)phenoxy)methyl)quinoline;

分子式：C25H20N4O

分子量：392.453

精确质量：392.164

Psa：52.83

密度：

简介：PF-2545920isadrugdevelopedbyPfizerforthetreatmentofschizophrenia.ItactsasaphosphodiesteraseinhibitorselectiveforthePDE10Asubtype.ThePDE10Aenzymeisexpressedprimarilyinthebrain,mostlyinthestriatum,nucleusaccumbensandolfactorytubercle,andisthoughttobeparticularlyimportantinregulatingtheactivityofdopamine-sensitivemediumspinyneuronsinthestriatumwhichareknowntobetargetsofconventionalantipsychoticdrugs.OlderPDE10Ainhibitorssuchaspapaverinehavebeenshowntoproduceantipsychoticeffectsinanimalmodels,andmorepotentandselectivePDE10Ainhibitorsareacurrentareaofresearchfornovelantipsychoticdrugswhichactthroughadifferentpathwaytoconventionaldopamineor5HT2Aantagonistdrugsandmayhaveamorefavourablesideeffectsprofile.PF-2545920iscurrentlyoneofthefurthestadvancedPDE10AinhibitorsindevelopmentandhasprogressedthroughtoPhaseIIclinicaltrialsinhumans.