メチルナルトレキソン臭化物
メチルナルトレキソン臭化物 物理性質
- 融点 :
- 237-239°C
- 貯蔵温度 :
- -20°C
- 溶解性:
- H2O: ≥5mg/mL
- 外見 :
- 粉
- 色:
- 白からベージュ
- 安定性::
- Hygroscopic
メチルナルトレキソン臭化物 価格
もっと(5)
メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
Sigma-Aldrich Japan
|
SML0277 |
≥97% (HPLC)
Methylnaltrexone bromide ≥97% (HPLC) |
73232-52-7 |
5mg |
¥22600 |
2024-03-01 |
購入 |
富士フイルム和光純薬株式会社(wako)
|
M-227 |
Methylnaltrexone bromide solution 1?mg/mL in methanol, certified reference material, ampule of 1?mL, Cerilliant?
1?mg/mL in methanol, certified reference material, ampule of 1?mL, Cerilliant? |
73232-52-7 |
1ML |
¥17000 |
2024-03-01 |
購入 |
Sigma-Aldrich Japan
|
1430735 |
United States Pharmacopeia (USP) Reference Standard
Methylnaltrexone bromide United States Pharmacopeia (USP) Reference Standard |
73232-52-7 |
100mg |
¥246000 |
2024-03-01 |
購入 |
Sigma-Aldrich Japan
|
1430724 |
United States Pharmacopeia (USP) Reference Standard
Methylnaltrexone Peak Identification Mixture Cll United States Pharmacopeia (USP) Reference Standard |
73232-52-7 |
10MG |
¥156800 |
2024-03-01 |
購入 |
Sigma-Aldrich Japan
|
SML0277 |
≥97% (HPLC)
Methylnaltrexone bromide ≥97% (HPLC) |
73232-52-7 |
25mg |
¥114000 |
2024-03-01 |
購入 |
メチルナルトレキソン臭化物 化学特性,用途語,生産方法
効能
便秘治療薬, オピオイド受容体拮抗薬
説明
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.
化学的特性
Pale Pink Solid
使用
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.
一般的な説明
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).
メチルナルトレキソン臭化物 上流と下流の製品情報
原材料
準備製品
メチルナルトレキソン臭化物 生産企業
Global( 77)Suppliers
73232-52-7(メチルナルトレキソン臭化物)キーワード:
- 73232-52-7
- 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
- メチルナルトレキソン臭化物
- メチルナルトレキソン臭化物 (JAN)