Description
Chlorpromazineisaphenothiazinethatexhibitsantipsychotic,antidepressant,anxiolytic,neuroprotective,andanticancerchemotherapeuticactivities.ChlorpromazineinhibitsD1/2/3/4receptors,5-HT1/2receptors,α1/2-adrenergicreceptors,andM1/2muscarinicacetylcholinereceptors(mAChRs).ChlorpromazinestABIlizesmisfoldingmotifsofprions,preventingoligomerization.Additionally,thiscompoundactsasafunctionalinhibitorofacidsphingomyelinase(FIASMA).Invivo,chlorpromazineinducesautophagyandapoptosis,inhibitinggrowthofgliomatumors.
References
BaralPK,SwayampakulaM,RoutMK,etal.Structuralbasisofprioninhibitionbyphenothiazinecompounds.Structure.2014Feb4;22(2):291-303.PMID:24373770.
RamosMA.Drugsincontext:ahistoricalperspectiveontheoriesofpsychopharmaceuticalefficacy.JNervMentDis.2013Nov;201(11):926-33.PMID:24177478.
ShinSY,LeeKS,ChoiYK,etal.TheantipsychoticagentchlorpromazineinducesautophagiccelldeathbyinhibitingtheAkt/mTORpathwayinhumanU-87MGgliomacells.Carcinogenesis.2013Sep;34(9):2080-9.PMID:23689352.
BaumeisterAA.Thechlorpromazineenigma.JHistNeurosci.2013;22(1):14-29.PMID:23323529.
KornhuberJ,MuehlbacherM,TrappS,etal.Identificationofnovelfunctionalinhibitorsofacidsphingomyelinase.PLoSOne.2011;6(8):e23852.PMID:21909365.
PeroutkaSJ,SynderSH.Relationshipofneurolepticdrugeffectsatbraindopamine,SEROtonin,alpha-adrenergic,andhistaminereceptorstoclinicalpotency.AmJPsychiatry.1980Dec;137(12):1518-22.PMID:6108081.
MasudaK,KimuraA,HaniehH,etal.ArylhydrocarbonreceptornegativelyregulatesLPS-inducedIL-6productionthroughsuppressionofhistamineproductioninmacrophages.IntImmunol.2011Oct;23(10):637-645.PMID:21930594.