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Merck
CN
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文件

安全信息

SML0277

Sigma-Aldrich

甲基纳曲酮 溴化物

≥97% (HPLC)

别名:

17-(Cyclopropylmethyl)-4,5α-epoxy-3,14-dihydroxy-17-methyl-6-oxomorphinanium bromide, MNTX, Methylnaltrexonium, Mrz-2663, N-Methylnaltrexone, Naltrexone MB, Quaternary ammonium naltrexone

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About This Item

经验公式（希尔记法）:
C21H26NO4 · Br
CAS号:
73232-52-7
分子量:
436.34
MDL编号:
MFCD06407831
UNSPSC代码:
12352200
PubChem化学物质编号:
329825285
NACRES:
NA.77

质量水平

100

检测方案

≥97% (HPLC)

形式

powder

储存条件

desiccated

颜色

white to beige

溶解性

H2O: ≥5 mg/mL

运输

wet ice

储存温度

−20°C

SMILES字符串

[Br-].C[N@+]1(CC[C@]23[C@H]4Oc5c(O)ccc(C[C@@H]1[C@]2(O)CCC4=O)c35)CC6CC6

InChI

1S/C21H25NO4.BrH/c1-22(11-12-2-3-12)9-8-20-17-13-4-5-14(23)18(17)26-19(20)15(24)6-7-21(20,25)16(22)10-13;/h4-5,12,16,19,25H,2-3,6-11H2,1H3;1H/t16-,19+,20+,21-,22?;/m1./s1

InChI key

IFGIYSGOEZJNBE-KNLJMPJLSA-N

基因信息

human ... OPRM1(4988)

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一般描述

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).

应用

Methylnaltrexone bromide has been used as a drug to measure plasma protein binding (PPB), permeability (Pm) and the membrane coefficient (KIAM) for the prediction of blood brain barrier (BBB) penetration. It is also used as a mu-opioid receptor (MOR) antagonist to abrogate morphine tolerance and opioid-induced hyperalgesia (OIH).

生化/生理作用

Methylnaltrexone bromide is a narcotic antagonist. It is a peripheral mu-opiod receptor antagonist that cannot cross the blood-brain barrier. It reverses many opioid side-effects without interfering with pain relief.

特点和优势

This compound is featured on the Opioid Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

象形图

Health hazard
GHS08

警示用语：

Warning

危险声明

H371

危险分类

STOT SE 2 Oral

靶器官

Gastrointestinal tract

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

法规信息

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A Brokjaer et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 27(5), 693-704 (2015-03-27)
Opioid antagonists are increasingly used to abolish the gastrointestinal side effects of opioids. However, they can potentially interfere with local analgesia exerted via opioid receptors in the gut. Thus, in the current study we aimed to explore the effect of
Neal E Slatkin et al.
Journal of pain and symptom management, 42(5), 754-760 (2011-11-03)
Methylnaltrexone is a selective peripherally acting mu-opioid receptor antagonist that decreases the constipating effects of opioids without affecting centrally mediated analgesia. In two double-blind, placebo-controlled, Phase III studies of methylnaltrexone for opioid-induced constipation in patients with advanced illness, abdominal pain
Antonio Gatti et al.
Clinical drug investigation, 32(5), 293-301 (2012-03-15)
Opioids are one of the most widely used therapies for the palliative treatment of cancer pain; however, despite their proven analgesic efficacy, they are associated with several adverse effects. Associated with psychological distress and multiple concomitant clinical concerns, constipation is
Lucas Anissian et al.
Journal of hospital medicine, 7(2), 67-72 (2011-10-15)
Methylnaltrexone has been shown to be effective for treating opioid-induced constipation (OIC) in chronic settings, but its effects on acute OIC have not been studied. To assess safety and efficacy of subcutaneous methylnaltrexone in patients with acute OIC after orthopedic
Expanding LogP: Present possibilities
Vraka C, et al.
Nuclear Medicine and Biology, 58, 20-32 (2018)
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