SKU: A172

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Description

Alvimopan is a gastroprokinetic peripherally restricted mu-opioid receptor antagonist (MOR). It has a favorable kinetic activity (0.2 ng/ml) and dissociates more slowly than most other ligands.

    CAS Number

    156053-89-3

    Molecular Formula

    C25H32N2O4

    Molecular Weight

    424.53

    Mechanism of Action

    Alvimopan competitively binds to the mu-opioid receptor in the gastrointestinal tract. It has a low systemic absorption and a high affinity for mu-opioid receptors. This compound assists gastrointestinal motility dysfunction.

    Storage Conditions

    2-8°C (protect from light)

    Tariff Code

    2933.39.4100

Applications

    Eukaryotic Cell Culture Applications

    In vitro studies with Alvimopan using CHO cell membranes revealed that it inhibited GTP binding with an IC50 of 1.7 nM.

Specifications

    Form

    Powder

    Appearance

    White to off-white powder

    Source

    Synthetic

References

    References

    Beattie DT (2007) The in vitro pharmacology of the peripherally restricted opioid receptor antagonists, Alvimopan, ADL 08-0011 and methylnaltrexone. Naunyn Schmiedebergs Arch Pharmacol. 375(3):205-220 PMID 17340127 Cassel JA, Daubert JD and DeHaven RN (2005) [(3)H] Alvimopan binding to the micro opioid receptor: comparative binding kinetics of opioid antagonists. Eur. J. Pharmacol 520(1-3):29-36 PMID 16165125 Camilleri M (2005) Alvimopan, a selective peripherally acting µ-opioid antagonist. Neurogastroenterol. & Motil. 172):157-165 Fukuda H (2006) The selective mu opioid receptor antagonist, Alvimopan, improves delayed GI transit of postoperative ileus in rats. Brain Res.102(1):63-70 PMID 16797494 Kaserer T et al (2016) μ Opioid receptor: novel antagonists and structural modeling. Sci. Rep 6:21548 PMID 26888328 Schmidt WK (2001) Alvimopan (ADL 8-2698) is a novel peripherla opioid antagonist. A. J. Surg. 182(5):S27-S38

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