MaslovLN,KhaliulinI,OeltgenPR,etal.ProspectsforCreationofCardioprotectiveandAntiarrhythmicDrugsBasedonOpioidReceptorAgonists.[J].Medicinalresearchreviews,,36(5):-.

Abstract:

Ithasnowbeendemonstratedthatthemu,delta1,delta2,andkappa1opioidreceptor(OR)agonistsrepresentthemostpromisinggroupofopioidsforthecreationofdrugsenhancingcardiactolerancetothedetrimentaleffectsofischemia/reperfusion(I/R).OpioidsareabletopreventnecrosisandapoptosisofcardiomyocytesduringI/Randimprovecardiaccontractilityinthereperfusionperiod.TheORagonistsexertaninfarct-reducingeffectwithprophylacticadministrationandpreventreperfusion-inducedcardiomyocytedeathwhenischemicinjuryofhearthasalreadyoccurred;thatis,opioidscanmimicpreconditioningandpostconditioningphenomena.Furthermore,opioidsarealsoeffectiveinpreventingischemia-inducedarrhythmias.

摘要:

已有的研究表明,阿片类药物中具有μ,δ1,δ2,κ1受体激动作用药物能显著增强心肌细胞对缺血再灌注(I/R)损伤的耐受能力。阿片类药物能抑制I/R时心肌细胞的坏死和凋亡并能改善再灌注时心肌的收缩力。不仅预防性给与阿片类药物能减少I/R时心肌的梗死面积,而且即使是缺血损伤发生后给与阿片类药物依然能降低再灌注损伤所导致的心肌坏死,换而言之,阿片类药物具有模拟“预处理”和“后处理”的作用。除此外,阿片类药物还具有抑制缺血所诱发的心律失常作用。









































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