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Merck
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文件

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號碼:
MFCD06407831
分類程式碼代碼:
12352200
PubChem物質ID:
329825285
NACRES:
NA.77

化驗

≥97% (HPLC)

形狀

powder

儲存條件

desiccated

顏色

white to beige

溶解度

H2O: ≥5 mg/mL

運輸包裝

wet ice

儲存溫度

−20°C

SMILES 字串

[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 密鑰

IFGIYSGOEZJNBE-KNLJMPJLSA-N

基因資訊

human ... OPRM1(4988)

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一般說明

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).

應用

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.

特點和優勢

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.

象形圖

Health hazard
GHS08

訊號詞

Warning

危險聲明

H371

危險分類

STOT SE 2 Oral

標靶器官

Gastrointestinal tract

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

分析证书(COA)

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Florian Pfab et al.
Current opinion in clinical nutrition and metabolic care, 15(2), 166-173 (2012-01-12)
Gastrointestinal motility disorders (GMDs) are common in the ICU. When encountering these problems, one typically thinks of prokinetics. This review summarizes current evidence of treatments. Prokinetics are not the first-line therapy for GMDs. In fact, the clinical implications of using
L Garten et al.
Archives of disease in childhood. Fetal and neonatal edition, 97(2), F151-F153 (2011-10-29)
Methylnaltrexone, a peripherally acting µ-opioid receptor antagonist, has been studied in adults for the treatment of opioid-induced constipation in advanced illness. Here, the authors document the first neonate to receive methylnaltrexone in an attempt to resolve morphine-induced urinary retention. An
Sergio B Sawh et al.
Mayo Clinic proceedings, 87(3), 255-259 (2012-03-06)
Gastrointestinal dysmotility and constipation are common problems in critical care patients. The majority of critical care patients are treated with opioids, which inhibit gastrointestinal (GI) motility and lead to adverse outcomes. We reasoned that methylnaltrexone (MNTX), a peripheral opioid antagonist
Edward Michna et al.
Pain medicine (Malden, Mass.), 12(8), 1223-1230 (2011-08-04)
Methylnaltrexone, a selective peripherally acting mu-opioid receptor antagonist, effectively treats opioid-induced constipation (OIC) in patients with advanced illness and shows efficacy in patients with chronic nonmalignant pain. The objective was to identify patients who achieved maximal treatment effect based on
Methylnaltrexone for treatment of opioid-induced constipation in advanced illness patients.
Slatkin N, et al.
The Journal of Supportive Oncology, 7(1), 39-46 (2009)
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