1. GPCR/G Protein
    Neuronal Signaling
  2. 5-HT Receptor
  3. Methylergometrine maleate

Methylergometrine maleate (Synonyms: Methylergonovine maleate; Ryegonovin; Spametrin F)

Cat. No.: HY-100988
Handling Instructions

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.

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Methylergometrine maleate Chemical Structure

Methylergometrine maleate Chemical Structure

CAS No. : 57432-61-8

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Description

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[1][2][3].

IC50 & Target[3]

serotonin

9.6 nM (pA2)

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[3].

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[2].

Molecular Weight

455.50

Formula

C₂₄H₂₉N₃O₆

CAS No.

57432-61-8

SMILES

[H][[email protected]]1(C2=C[[email protected]@H](C(N[[email protected]](CO)CC)=O)CN1C)CC3=CNC4=C3C2=CC=C4.OC(/C=C\C(O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

MethylergometrineMethylergonovine Ryegonovin Spametrin F5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorAntihemorrhagicuterotonicdopaminergicmigrainemethysergideergotalkaloid5-HT1BvasoconstrictorInhibitorinhibitorinhibit

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Methylergometrine maleate
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HY-100988
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