Description
Bupropionisanantidepressantthatisalsocommonlyusedasasmokingcessationaid.Thiscompoundhasadditionaltherapeuticpotential,asitpromotesmodestweightloss,showsefficacyasanADHDtreatment,andmayalsobeaneffectivetreatmentforneuropathicpain.BupropionisaDAandNEreuptakeinhibitor,decreasingthefiringrateofNEneuronsduetoactivationoftheirinhibitorysomatodendriticα2-adrenoreceptorsbycirculatingNE;bupropion’seffectsonNEreuptakearesomewhatstrongerthanitseffectsonDAreuptake.Additionally,bupropionisanoncompetitiveantagoNISTatα3β2,α3β4,α4β2nicotinicacetylcholinereceptors(nAChRs),decreasingtheprobABIlityofchannelopeninginclosednAChRsandacceleratingdesensitizationinopennAChRs.
References
ShahTH,MorADImehrA.Bupropionforthetreatmentofneuropathicpain.AmJHospPalliatCare.2010Aug;27(5):333-6.PMID:20185402.
AriasHR.Istheinhibitionofnicotinicacetylcholinereceptorsbybupropioninvolvedinitsclinicalactions?IntJBiochemCellBiol.2009Nov;41(11):2098-108.PMID:19497387.
LiZ,MaglioneM,TuW,etal.Meta-analysis:pharmacologictreatmentofobesity.AnnInternMed.2005Apr5;142(7):532-46.PMID:15809465.
MillerDK,SumithranSP,DwoskinLP.Bupropioninhibitsnicotine-evoked[(3)H]overflowfromratstriatalslicespreloadedwith[(3)H]dopamineandfromrathippocampalslicespreloadedwith[(3)H]norepinephrine.JPharmacolExpTher.2002Sep;302(3):1113-22.PMID:12183670.
DongJ,BlierP.ModificationofnorepinephrineandSEROtonin,butnotdopamine,neuronfiringbysustainedbupropiontreatment.Psychopharmacology(Berl).2001Apr;155(1):52-7.PMID:11374336.
CantwellDP.ADHDthroughthelifespan:theroleofbupropionintreatment.JClinPsychiatry.1998;59Suppl4:92-4.PMID:9554326.