Naltrexone methylbromide
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- CAS-Nr.
- 73232-52-7
- Englisch Name:
- Naltrexone methylbromide
- Synonyma:
- MNTX;Moa-728;Relistor;Unii-rfo6il3D3m;Adamantane Impurity 52;Naltrexone methobromide;Methylnaltrexone bromide;Naltrexone methylbromide;Methyhaaltrexone broMide;N-Methyl Naltrexone BroMide
- CBNumber:
- CB11105859
- Summenformel:
- C21H26BrNO4
- Molgewicht:
- 436.35
- MOL-Datei:
- 73232-52-7.mol
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Naltrexone methylbromide Eigenschaften
- Schmelzpunkt:
- 237-239°C
- storage temp.
- -20°C
- L?slichkeit
- H2O: ≥5mg/mL
- Aggregatzustand
- powder
- Farbe
- white to beige
- Stabilit?t:
- Hygroscopic
Naltrexone methylbromide Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
The widespread efficacy of opioids in treating patients with moderate to
severe acute and chronic pain is often accompanied by untoward side
effects. In particular, opioid-induced bowel dysfunction is one of the
more common and debilitating consequences afflicting up to 50% of
patients. To counteract the peripherally-mediated adverse effects, opioid
antagonists such as naloxone, naltrexone, and nalmephene are sometimes prescribed. The latest market entry exploits a strategic
modification of naltrexone to lower its lipid solubility and increase its
polarity: quaternization of the amine of naltrexone by methylation
(methyl bromide) prevents crossing of the blood–brain barrier thereby
creating an effective peripheral antagonist. Despite a loss of potency
upon methylation, methylnaltrexone antagonizes opioid binding at
m-opioid receptors with an IC
50 of 70 nM. Its affinity for k-opioid receptors
is approximately eightfold less (IC
50＝ 575 nM) with no significant binding
to d-opioid, orphanin, or non-opioid receptors. Methylnaltrexone bromide
has been approved for the treatment of opioid-induced constipation in
patients with advanced illness receiving palliative care.Regarding metabolism, methylnaltrexone bromide is eliminated primarily as intact drug (85% based on administered radioactivity) by slightly more renal than hepatic clearance.
The most common adverse events were abdominal pain and flatulence followed by nausea, dizziness, and diarrhea.
Chemische Eigenschaften
Pale Pink Solid
Verwenden
A metabolite of Naltrexone (N285750). Methylnaltrexone (MNTX), a selective μ-opioid receptor antagonist, functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.
Allgemeine Beschreibung
Methylnaltrexone does not cross blood brain barrier and does not affect the opioid effects in the brain, such as analgesia. It is used to treat opioid-induced constipation (OIC).
Naltrexone methylbromide Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Naltrexone methylbromide Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.
Global( 76)Lieferanten
- Naltrexone methobromide
- Naltrexone methylbromide
- Moa-728
- Morphinanium, 17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-17-methyl-6-oxo-, bromide, (5alpha)-
- Relistor
- Unii-rfo6il3D3m
- Methylnaltrexone bromide
- (5alpha)-17-(Cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-17-methyl-6-oxomorphinanium bromide
- N-Methyl Naltrexone BroMide
- (5α)-17-(CyclopropylMethyl)-4,5-epoxy-3,14-dihydroxy-17-Methyl-6-oxoMorphinaniuM BroMide
- N-CyclopropylMethyl-noroxyMorphone MethobroMide
- Methyhaaltrexone broMide
- 17-(CyclopropylMethyl)-4,5-epoxy-3,14-dihydroxy-17-Methyl-6-oxoMorphinaniuM broMide
- MNTX
- Quaternary ammonium naltrexone
- 17-(Cyclopropylmethyl)-4,5A-Epoxy-3,14-Dihydroxy-17-Methyl-6-Oxomorphinanium Bromide
- Methylnaltrexone Peak Identification Mixture Cll
- (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
- Methylnaltrexone iodide salt
- N-Methyl Naltrexone Bromide (1.0mg/ml in DMSO)
- Methylnaltrexone Bromide (1430735)
- inhibit,Opioid Receptor,suppression,gastrointestinal,Methylnaltrexone bromide,blood-brain,tract,peripheral,barrier,analgesia,Inhibitor
- Adamantane Impurity 52
- 73232-52-7
- C21H26NO4Br
- Aromatics
- Heterocycles
- Intermediates & Fine Chemicals
- Metabolites & Impurities
- Pharmaceuticals
