生物活性Methylergometrinemaleate(Methylergonovinemaleate)是一种麦角生物碱,是一种具有血管收缩和子宫收缩作用的Methysergide的活性代谢产物。Methylergometrinemaleate是一种有效的,选择性的,具有口服活性的5-HT受体拮抗剂,pA2值为9.6。Methylergometrinemaleate具有抗偏头痛和多巴胺能活性,可用于预防和控制产后出血。靶点serotonin9.6nM(pA2)体外研究BothMethysergideandMethylergometrinedisplacetheconcentration-responsecurveof5-HTtotherightanddepressedthemaximumeffect;thus,bothagentsbehavedasnon-competitiveantagonistsof5-HT.Methylergometrineisapproximately40-timesmorepotentthanMethysergideasanantagonistofthe5-HT-inducedresponses,sincethecalculatedapparentpA2valuesare9.6and8.0,respectively.体内研究MethylergometrineismorepotentthanMethysergideasavasoconstrictoronbovinemiddlecerebralarteryandhumancoronaryarteries,aneffecton5-HT1Breceptors.SubacuteoraladministrationwouldresultinmetabolismofMethysergidetoMethylergometrine.
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