CAS:61413-54-5
61413-54-5
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.
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