Description
IstradefyllineisacompetitiveinhibitorofadenosineA2Areceptorsthatexhibitstremorlyticactivity.IstradefyllineiscurrentlyunderexaminationasapotentialtreatmentforParkinson’sdisease,asitdecreases“off”timeinsubjectswithParkinson’sdiseasewithoutworseningdyskinesia.Istradefyllineincreasesdopaminelevelsinnormaland6-OHDA-lesionedanimalmodels,improvingcognitiveperformance.Inotheranimalmodels,istradefyllinedecreasesGABAreleaseandelicitsconditionedplacepreference(CPP)andincreaseslocomotoractivity,indicatingapotentialroleforadenosinereceptorsinrewardandreinforcement.
References
KadowakiHoritaT,KobayashiM,MoriA,etal.EffectsoftheadenosineA2AantagoNISTistradefyllineoncognitiveperformanceinratswitha6-OHDAlesioninprefrontalcortex.Psychopharmacology(Berl).2013Dec;230(3):345-52.PMID:23748382.
SakiM,YamadaK,KoshimuraE,etal.InvitropharmacologicalprofileoftheA2Areceptorantagonististradefylline.NaunynSchmiedebergsArchPharmacol.2013Nov;386(11):963-72.PMID:23812646.
MizunoY,HasegawaK,KondoT,etal.Clinicalefficacyofistradefylline(KW-6002)inParkinson"sdisease:arandomized,controlledstudy.MovDisord.2010Jul30;25(10):1437-43.PMID:20629136.
SalamoneJD,BetzAJ,IshiwariK,etal.TremorolyticeffectsofadenosineA2Aantagonists:implicationsforparkinsonism.FrontBiosci.2008May1;13:3594-605.PMID:18508458.
HarperLK,BeckettSR,MarsdenCA,etal.EffectsoftheA2AadenosinereceptorantagonistKW6002inthenucleusaccumbensinvitroandinvivo.PharmacolBiochemBehav.2006Jan;83(1):114-21.PMID:16451807.