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Methylnaltrexone (bromide)

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    Methyl<wbr/>naltrexone (bromide)
  • Methyl<wbr/>naltrexone (bromide)
Cat No: 24072
Biochemicals - Receptor Pharmacology
Cayman

Methylnaltrexone is a quaternary positively-charged form of naltrexone (Item No. 15520) that does not cross the blood brain barrier. It is a peripherally restricted µ-opioid receptor antagonist with a Ki value of 10 nM for human recombinant receptors ...

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This product can only be bought through Cayman Chemical. Please contact us.

Territorial Availability: Available through Bertin Technologies only in France
Synonyms:
  • 17-(cyclopropylmethyl)-4,5?-epoxy-3,14-dihydroxy-17-methyl-6-oxo-morphinanium, monobromide
Correlated keywords:
  • 83387-25-1 MNTX MRZ2663BR methobromide Relistor
Product Overview:
Methylnaltrexone is a quaternary positively-charged form of naltrexone (Item No. 15520) that does not cross the blood brain barrier. It is a peripherally restricted µ-opioid receptor antagonist with a Ki value of 10 nM for human recombinant receptors expressed in CHO-K1 cells and IC50 values of 130.7 and 0.43 nM in rat brain membranes prepared with sodium chloride or water, respectively.{41513} Methylnaltrexone is selective for µ-opioid receptors over δ- and κ-opioid receptors (Kis = 630.95 and 31.62 nM, respectively). It inhibits contractions evoked by electrical field stimulation (EFS) in ileum isolated from morphine-naïve guinea pigs and dose-dependently decreases spontaneous mechanical activity in ileum isolated from morphine-treated guinea pigs when administered at doses of 1 and 10 µM.{41514} It does not inhibit heroin self-administration in rats and does not induce withdrawal syndrome in morphine-dependent rhesus monkeys when administered at doses up to 32 mg/kg.{41513,41515} Formulations containing methylnaltrexone have been used in the treatment of opioid-induced constipation.
Size 1 mg
Shipping dry ice
CAS Number 73232-52-7
Molecular Formula C21H26NO4 • Br
SMILES O[C@]12[C@]3(CC[N@+](CC4CC4)(C)[C@@H]2C5)[C@](OC6=C3C5=CC=C6O)([H])C(CC1)=O.[Br-]
Molecular Weight 436,3
Formulation A crystalline solid
Purity ≥95%
Custom Code 2907.19
UNSPSC code 12352100

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

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ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.

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