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Methylergometrine maleate

CAS No. : 57432-61-8

MCE 站：Methylergometrine maleate

产品活性：Methylergometrine maleate (Methylergonovine maleate) 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。Methylergometrine maleate 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。Methylergometrine maleate 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。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor

In Vitro: Both Methysergide and Methylergometrine displace the concentration-response curve of 5-HT to the right and depressed the maximum effect ; thus, both agents behaved as non-competitive antagonists of 5-HT. Methylergometrine is approximately 40-times more potent than Methysergide as an antagonist of the 5-HT-induced responses, since the calculated apparent pA2 values are 9.6 and 8.0, respectively.

In Vivo: Methylergometrine is more potent than Methysergide as a vasoconstrictor on bovine middle cerebral artery and human coronary arteries, an effect on 5-HT1B receptors. Subacute oral administration would result in metabolism of Methysergide to Methylergometrine.

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