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Merck

SML0277

Sigma-Aldrich

Methylnaltrexone bromide

≥97% (HPLC)

別名:

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

実験式(ヒル表記法):
C21H26NO4 · Br
CAS番号:
分子量:
436.34
MDL番号:
UNSPSCコード:
12352200
PubChem Substance ID:
NACRES:
NA.77

品質水準

アッセイ

≥97% (HPLC)

フォーム

powder

保管条件

desiccated

white to beige

溶解性

H2O: ≥5 mg/mL

輸送温度

wet ice

保管温度

−20°C

SMILES記法

[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

遺伝子情報

human ... OPRM1(4988)

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詳細

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).

アプリケーション

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).

生物化学的/生理学的作用

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.

特徴および利点

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.

ピクトグラム

Health hazard

シグナルワード

Warning

危険有害性情報

危険有害性の分類

STOT SE 2 Oral

ターゲットの組織

Gastrointestinal tract

保管分類コード

11 - Combustible Solids

WGK

WGK 3

引火点(°F)

Not applicable

引火点(℃)

Not applicable


適用法令

試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。

Jan Code

SML0277-5MG:
SML0277-BULK:
SML0277-VAR:
SML0277-25MG:


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文書ライブラリにアクセスする

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)
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
Danial E Baker
Reviews in gastroenterological disorders, 9(3), E84-E93 (2009-11-10)
Constipation is a common problem associated with opiates and opioid compounds used for the treatment of pain and other medical conditions, and can influence patient quality of life. Methylnaltrexone appears effective in the therapy of opioid-induced constipation and will be
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

資料

We offers many products related to opioid receptors for your research needs.

We offers many products related to opioid receptors for your research needs.

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