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.
|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.|
|Purity Level||98.0%-102.0% (anhydrous basis)02.0% (anhydrous basis)|
|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.|
|Solubility||Slightly soluble in DMSO. Very slightly soluble in water.|
|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|