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Merck
CN

SML0277

甲基纳曲酮 溴化物

≥97% (HPLC), narcotic antagonist, powder

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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关于此项目

经验公式（希尔记法）:
C21H26NO4 · Br
化学文摘社编号:
73232-52-7
分子量:
436.34
UNSPSC Code:
12352200
PubChem Substance ID:
329825285
NACRES:
NA.77
MDL number:
MFCD06407831

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产品名称

甲基纳曲酮 溴化物, ≥97% (HPLC)

SMILES string

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

InChI key

IFGIYSGOEZJNBE-KNLJMPJLSA-N

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

assay

≥97% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

H2O: ≥5 mg/mL

shipped in

wet ice

storage temp.

−20°C

Quality Level

100

Gene Information

human ... OPRM1(4988)

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相关类别

General description

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).

Application

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).

Biochem/physiol Actions

Methylnaltrexone bromide is a narcotic antagonist.
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.

Features and Benefits

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.

pictograms

Health hazard
GHS08

signalword

Warning

hcodes

H371

Hazard Classifications

STOT SE 2 Oral

target_organs

Gastrointestinal tract

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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历史批次信息供参考:

分析证书(COA)

Lot/Batch Number
0000368079
0000368079
0000189929
0000189930
0000187274

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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
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
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
Loss of mu-opioid receptor signaling in nociceptors, but not microglia, abrogates morphine tolerance without disrupting analgesia
Corder G, et al.
Nature Medicine, 23(2), 164-164 (2017)
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