- 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.
M.W.275.34
C16H21NO3
[61413-54-5]
M.I.14:8251
Storage
Storeatorbelow-20ºC
Solubility
SolubleinDMSOat50mg/mL;solubleinethanolat25mg/mLwithwarming;verypoorlysolubleinwater;maximumsolubilityinplainwaterisestimatedtobeabout50-100µM;buffers,serum,orotheradditivesmayincreaseordecreasetheaqueoussolubilit
Disposal
A
LC Laboratories公司提供信号转导,调节蛋白亚细胞定位试剂(抗生素)产品蛋白抑制剂产品。热门产品 Bortezomib硼替佐米(99%,97%) Cyclosporine-A环胞霉素A Cyclopamine环巴胺 17-DMAG,Hydrochloride Salt HSP90抑制剂 Everolimus依维莫司 FK-506他克莫司 Forskolin腺苷酸环化酶激活剂 Gefitinib吉非替尼 Leptomycin B细霉素B出核转运抑制剂 LY 294002 PI3-K抑制剂 PD98059 MEK抑制剂 RoscovitineCDK抑制剂 Rapamycin雷帕霉素 SB 202190 MAPK抑制剂 SB203580 P38MAPK抑制剂 SP600125 JNK抑制剂 Staurosporine星孢菌素 UO126 MAPK抑制剂