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 Purity: 99.76%
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.

For research use only. We do not sell to patients.

Methylergometrine maleate Chemical Structure

Methylergometrine maleate Chemical Structure

CAS No. : 57432-61-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 143 In-stock
Estimated Time of Arrival: December 31
5 mg USD 130 In-stock
Estimated Time of Arrival: December 31
10 mg USD 230 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
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
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (219.54 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1954 mL 10.9769 mL 21.9539 mL
5 mM 0.4391 mL 2.1954 mL 4.3908 mL
10 mM 0.2195 mL 1.0977 mL 2.1954 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

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

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Product Name:
Methylergometrine maleate
Cat. No.:
HY-100988
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