Inhibitors Product Data Sheet
Methylergometrine maleate • Agonists
Cat. No.: HY-100988 CAS No.: 57432-61-8
Molecular Formula: C₂₄H₂₉N₃O₆ •
Molecular Weight: 455.5 Screening Libraries Target: 5-HT Receptor Pathway: GPCR/G Protein; Neuronal Signaling 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)
Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 2.1954 mL 10.9769 mL 21.9539 mL Stock Solutions 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
BIOLOGICAL ACTIVITY
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 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
Page 1 of 2 www.MedChemExpress.com 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.
REFERENCES
[1]. Meneghetti F, et al. Crystallographic and NMR Investigation of Ergometrine and Methylergometrine, Two Alkaloids from Claviceps purpurea. Molecules. 2020 Jan 14;25(2). pii: E331.
[2]. Koehler PJ, et al. History of methysergide in migraine. Cephalalgia. 2008 Nov;28(11):1126-35.
[3]. Tfelt-Hansen P, et al. Methylergometrine antagonizes 5 HT in the temporal artery. Eur J Clin Pharmacol. 1987;33(1):77-9.
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Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA
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