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编 号:F394410
分子式:C24H29N3O6
分子量:455.5
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10mM*1mL in DMSO
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5mg
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10mg
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生物活性:
Methylergometrine maleate (Methylergonovine maleate) is an ergot alkaloid and an active metabolite of Methysergide with vasoconstrictive and uterotonic activity. Methylergometrine maleate is a potent, selective and orally active 5-HT receptors antagonist with a pA2 value of 9.6. Methylergometrine maleate has antimigraine and dopaminergic activity. Methylergometrine maleate can used for the prevention and control of postpartum hemorrhage.

体内研究:
作为牛大脑中动脉和人类冠状动脉的血管收缩剂,甲基麦角新碱比麦角新碱更有效,对 5-HT1B 受体有影响。亚急性口服给药会导致美西麦角新陈代谢为美麦角新碱。

体外研究:
Methysergide 和 Methylergometrine 都使 5-HT 的浓度-反应曲线向右移动并抑制了最大效应;因此,两种药物均表现为 5-HT 的非竞争性拮抗剂。作为 5-HT 诱导反应的拮抗剂,Methylergometrine 的效力大约是 Methysergide 的 40 倍,因为计算的表观 pA2 值分别为 9.6 和 8.0。
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