代谢

CAS号：61413-54-5

品名：咯利普兰rolipram

中文别名：(±)-Rolipram;诺普利兰;4-[3-(环戊氧基)-4-甲氧基苯基]-2-吡咯烷酮;4-[3-(环戊基氧基)-4-甲氧基苯基]-2-吡咯烷二酮;

英文别名：EINECS262-771-1;Rolipramum[Latin];Adeo;Rolipram;4-(3-cyclopentyloxy-4-methoxyphenyl)pyrrolidin-2-one;[3H]-Rolipram;4-[3-(cyclopentyloxy)-4-methoxyphenyl]-2-pyrrolidinone;4-(3-cyclopentyloxy-4-methoxy-phenyl)-pyrrolidin-2-one;

分子式：C16H21NO3

分子量：275.343

精确质量：275.152

Psa：47.56

MDL号：MFCD00270906

外观与性状：固体

密度：1.155 g/cm3

沸点：472.7ºC at 760 mmHg

熔点：127-133ºC

闪点：239.7ºC

折射率：1.552

储存条件：0-6ºC

安全说明：S26; S36

危险类别码：R36/37/38

海关编码：2933790090

危险品运输编码：UN 3249

危险类别：6.1(b)

包装等级：III

危险品标志：Xi

简介：Rolipramisaselectivephosphodiesterase-4inhibitordiscoveredanddevelopedbyScheringAGasapotentialantidepressantdrugintheearly1990s.Itservedasaprototypemoleculeforseveralcompanies'drugdiscoveryanddevelopmentefforts.:668ffRolipramwasdiscontinuedafterclinicaltrialsshowedthatitstherapeuticwindowwastoonarrow;itcouldnotbedosedathighenoughlevelstobeeffectivewithoutcausingsignificantgastrointestinalsideeffects.:668;Rolipramhasseveralactivitiesthatmakeitacontinuingfocusforresearch.Theetiologyofmanyneurodegenerativediseasesinvolvesmisfoldedandclumpedproteinswhichaccumulateinthebrain.Cellshaveamechanismtodisposeofsuchproteinscalledtheproteasome.However,inAlzheimer'sdiseaseandsomeotherconditionstheactivityoftheseproteasomesisimpairedleadingtoabuildupoftoxicaggregates.Researchinmicesuggeststhatrolipramhastheabilitytorampuptheactivityofproteasomesandreducetheburdenoftheseaggregates.Preliminaryevidencesuggeststhatthiscanimprovespatialmemoryinmiceengineeredtohaveaggregatebuild-up.Itcontinuestobeusedinresearchasawell-characterizedPDE4inhibitor.:669IthasbeenusedinstudiestounderstandwhetherPDE4inhibitioncouldbeusefulinautoimmunediseases,Alzheimer'sdisease,cognitiveenhancement,spinalcordinjury,andrespiratorydiseaseslikeasthmaandCOPD.