LC Labs/R-2020 (R,S)-Rolipram, >99%/R-2020/1 g

• Rolipramisaselectivephosphodiesterase4(PDE4)inhibitor.PDE4enzymesinactivatecyclicAMP(cAMP)viahydrolysisto5"-AMP.
• Rolipramhastwoenantiomericforms,R(-)andS(+).Thisproductistheracemicmixtureofthetwoenantiomers.
• R-(-)-rolipramdemonstratedahigheraffinityforthePDE4enzymethanS-(+)-rolipram,byabout8-foldinvitroandabout12-to15-foldinvivo.Parker,C.A.,etal."Behaviourof[11C]R(-)-and[11C]S(+)-rolipraminvitroandinvivo,andtheiruseasPETrADIotracersforthequantificativeassayofPDE4."Synapse55:270-279(2005).
• Rolipramisabletoreverseischemia-reperfusion(I/R)-inducedincreasedmicrovascularpermeABIlitythroughcAMPphosphodiesterase(PDE)isozyme-selectiveinhibition.Barnard,J.W.,etal."Reversalofpulmonarycapillaryischemia-reperfusioninjurybyrolipram,acAMPphosphodiesteraseinhibitor."J.Appl.Physiol.77:774-781(1994).
• Rolipramreducedtheinitialandlateresponsetoovalbumin(OVA)inisolatedstripsofguinea-pigcolonicsmoothmuscle.Forbothresponses,the(S)-isomer(EC50=approximately1.0µM)wasabout10foldlesspotentthanthe(R)-isomer(EC50=approximately0.1µM).Grous,M.andBarnette,M."Preventionbyphosphodiesteraseinhibitorsofantigen-inducedcontractionofguinea-pigcolonicsmoothmuscle."Br.J.Pharmacol.111:259-263(1994).
• Rolipramsuppressedcardiopulmonarybypass-inducedsystemicinflammatoryresponsesyndrome,probablythroughtheregulationofproinflammatorymediatorsbyinhibitingphosphodiesterasetype4.Hamamoto,M.,etal."Suppressiveeffectofphosphodiesterasetype4inhibitiononsystemicinflammatoryresponsesaftercardiopulmonarybypass."J.Artif.Organs9:144-148(2006).
• R6/2mutantmicerecapitulatehumanHuntington"sdiseaseinmanyways.Rolipramhasaneuroprotectiveeffectinthesemice.Aftertreatmentwithrolipram,R6/2micesurvivedlongeranddisplayedlessseveresignsofneurologicaldysfunction.DeMarch,Z.,etal."BeneficialeffectsofrolipramintheR6/2mousemodelofHuntington"sdisease."Neurobiol.Dis.30:375-387(2008).
• Dopamineplaysanessentialroleintheregulationofmotorandcognitivefunctions.TheeffectofdopaminelargelydependsonthecAMP/PKAsignalingcascade.Rolipramshowsutilityinneuropsychiatricandneurodegenerativedisorders,posisblybyaffectingdopamineneurotransmission.Nishi,A.,etal."DistinctrolesofPDE4andPDE10AintheregulationofcAMP/PKAsignalinginthestriatum."J.Neurosci.28:10460-10471(2008).
• AnotherCASnumberpreviouslyassignedtorolipram,namely85416-74-6,hasbeendeletedbyCASandisnolongerinuse.
• Soldforlaboratoryormanufacturingpurposesonly;notforhuman,veterinary,food,orhouseholduse.
• ThisproductisofferedforR&Duseinaccordancewith(i)35USC271(e)+A13(1)intheU.S.;(ii)Section69.1ofJapanesePatentLawinJapan;(iii)Section11,No.2oftheGermanPatentActof1981inGermany;(iv)Section60,Paragraph5boftheU.K.PatentsActof1977intheU.K.;(v)Sections55.2(1)and55.2(6)andothercommonlawexemptionsofCanadianpatentlaw;(vi)Section68BofthePatentsActof1953inNewZealandtogetherwiththeamendmentofsamebytheStatutesAmendmentBillof2002;(vii)suchrelatedlegislationand/orcaselawasmaybeorbecomeapplicableintheaforementionedcountries;and(viii)suchsimilarlawsandrulesasmayapplyinvariousothercountries.
• Notavailableinsomecountries;notavailabletosomeinstitutions;notavailableforsomeuses.

Storage

Solubility

Disposal