其他分子
CAS号：82159-09-9
品名：依帕司他epalrestat
中文别名：益帕瑞司特;依帕斯他;
英文别名：5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineaceticacid;Kinedak;2-[(5Z)-5-[(E)-2-methyl-3-phenylprop-2-enylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]aceticacid;(Z,E)-5-(2-methyl-3-phenyl-2-propenylidene)-4-oxo-2-thioxothiazolidine-3-aceticacid;Epalrestat;Ono2235;(Z,E)-5-(2-methyl-3-phenyl-2-propenylidene)-4-oxo-2-thioxo-3-thiazolidineaceticacid;
分子式：C15H13NO3S2
分子量：319.399
精确质量：319.034
Psa：115.0
MDL号：MFCD00865484
密度：1.43 g/cm3
沸点：516.8ºC at 760 mmHg
熔点：210-217ºC
闪点：266.4ºC
折射率：1.705
储存条件：通风低温干燥,与库房食品原料分开存放
简介：Epalrestatisacarboxylicacidderivativeandanoncompetitiveandreversiblealdosereductaseinhibitorusedforthetreatmentofdiabeticneuropathy,whichisoneofthemostcommonlong-termcomplicationsinpatientswithdiabetesmellitus.Itreducestheaccumulationofintracellularsorbitolwhichisbelievedtobethecauseofdiabeticneuropathy,retinopathyandnephropathyItiswelltolerated,withthemostcommonlyreportedadverseeffectsbeinggastrointestinalissuessuchasnauseaandvomiting,aswellasincreasesincertainliverenzymes.Chemically,epalrestatisunusualinthatitisadrugthatcontainsarhodaninegroup.Aldosereductaseisthekeyenzymeinthepolyolpathwaywhoseenhancedactivityisthebasisofdiabeticneuropathy.Aldosereductaseinhibitors(ARI)targetthisenzyme.OutofthemanyARIsdeveloped,ranirestatandfidarestatareinthetrialstage.Othershavebeendiscardedduetounacceptableadverseeffectsorweakefficacy.EpalrestatistheonlyARIcommerciallyavailable.Itiseasilyabsorbedintotheneuraltissueandinhibitstheenzymewithminimumsideeffects.
用途：醛糖还原酶抑制剂，能可逆性地抑制将葡萄糖转化为山梨醇的醛糖还原酶而发挥作用。用于糖尿病性神经末梢障碍造成的自觉症状、振动感觉异常、心跳变动异常的改善。用于预防和治疗糖尿病。
