推荐产品
质量水平
方案
≥97% (HPLC)
表单
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.
警示用语:
Warning
危险声明
危险分类
STOT SE 2 Oral
靶器官
Gastrointestinal tract
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
从最新的版本中选择一种:
分析证书(COA)
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
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
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
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
Methylnaltrexone for treatment of opioid-induced constipation in advanced illness patients.
The Journal of Supportive Oncology, 7(1), 39-46 (2009)
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