Methylnaltrexone Bromide is an antagonist of mu-opioid receptors (MOR) with IC50 value of 75nM.
MOR are a class of opioid receptors with high affinity for enkephalins and beta-endorphin but low affinity for dynorphins. Activation of MOR in the intestinal tract inhibits peristaltic action which causes constipation [1].
In patients with constipation, Methylnaltrexone Bromide plus standard care relieved the constipation symptoms with less time (38 days) and improved quality life of 0.02 years or 8.8 days [1]. Methylnaltrexone is a novel MOR antagonist, which does not pass the blood brain barrier. In the first two weeks of usage, Methylnaltrexone Bromide caused laxation in less than 24 hours for at least half of those patients without impairing pain control or causing serious adverse effects. In phase II studies, all 22 patients had fast laxation [2].
References:
[1]. Earnshaw SR, Klok RM, Iyer S, et al. Methylnaltrexone bromide for the treatment of opioid-induced constipation in patients with advanced illness--a cost-effectiveness analysis. Aliment Pharmacol Ther, 2010, 31(8): 911-921.
[2]. Bader S, Jaroslawski K, Blum HE, et al. Opioid-induced constipation in advanced illness: safety and efficacy of methylnaltrexone bromide. Clin Med Insights Oncol, 2011, 5: 201-211.
Methylnaltrexone Bromide
Catalog No.: GC16177Synonyms: MRZ 2663BR, Naltrexone methylbromide
Antagonist of peripherally acting μ-opioid
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 73232-52-7
5mgIn Stock
$37.00
1
25mgIn Stock
$141.00
1
50mgIn Stock
$260.00
1
100mgIn Stock
$402.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 5mg | $37.00 | In Stock | 1 | |
| 25mg | $141.00 | In Stock | 1 | |
| 50mg | $260.00 | In Stock | 1 | |
| 100mg | $402.00 | In Stock | 1 |
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Nature641, 529–536 (2025)
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Cell187(9):2288-2304 (2024)
Cell183(7):1867-1883 (2020)
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Description
Product Documents
Appearance:A solid
Chemical Properties
CAS No.
73232-52-7
Synonyms
MRZ 2663BR, Naltrexone methylbromide
Chemical Name
(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-3-methyl-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-3-ium-7-one;bromide
SMILES
C[N+]1(CCC23C4C(=O)CCC2(C1CC5=C3C(=C(C=C5)O)O4)O)CC6CC6.[Br-]
Molecular Formula
C21H26BrNO4
Molecular Weight
436.34
Solubility
PBS (pH 7.2): 10 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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