Alvimopan

Catalog No.S5935 Synonyms: LY 246736, ADL 8-2698

For research use only.

Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.

Alvimopan Chemical Structure

CAS No. 156053-89-3

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Biological Activity

Description Alvimopan (LY 246736, ADL 8-2698) is a potent, relatively nonselective opioid antagonist with Ki values of 0.77, 4.4, and 40 nM for the μ, δ, and κ opioid receptors, respectively, displaying >100-fold selectivity over other aminergic G-protein-coupled receptors.
Targets
μ-opioid receptor [1]
(Cell-free assay)
δ-opioid receptor [1]
(Cell-free assay)
δ-opioid receptor [1]
(Cell-free assay)
κ-opioid receptor [1]
(Cell-free assay)
0.77 nM(Ki) 4.4 nM 4.4 nM(Ki) 40 nM(Ki)
In vitro

Alvimopan is highly selective (by ≥227-fold) for the human μ receptor over the κ subtype, but has a more modest (≥6-fold) μ/δ receptor selectivity. In the guinea pig isolated ileum, alvimopan is a potent antagonist of morphine, DAMGO or endomorphin-1-induced, and μ opioid receptor-mediated, inhibition of electrically-evoked contractions (pA2 values of 9.6 or 9.7). The δ and κ antagonist potencies of alvimopan are lower in the guinea pig ileum (pA2 values of 8.7 and 7.8, respectively). Alvimopan (1 or 10 μM) has no significant affinity for a broad range of non-opioid receptors, ion channels and enzymes at which it has been tested[2].

In vivo

In animals, alvimopan antagonizes centrally mediated, morphine-induced analgesia only at relatively high doses, with very high plasma concentrations needed to cross the blood-brain barrier. After intravenous administration, alvimopan is approximately 200-times more potent at blocking peripheral verses central μ-receptors. After oral administration, alvimopan is also highly active. In dogs, intravenous administration of alvimopan provided dose-dependent increases in peak plasma concentrations and plasma area under the concentration-time curve. However, as a result of poor systemic absorption, oral doses up to 100 mg/kg produced low plasma concentrations (mean Cmax =92.9 ng/ml), which resulted in an oral bioavailability of approximately 0.03%. The half-life of alvimopan is estimated to be approximately 10 min after intravenous administration in dogs and rabbits[1].

Protocol (from reference)

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 424.53
Formula

C25H32N2O4

CAS No. 156053-89-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03068975 Terminated Drug: Alvimopan|Drug: Placebo Post Operative Ileus University of Puerto Rico|Merck Sharp & Dohme LLC September 1 2017 Phase 4
NCT00259922 Completed Drug: Placebo|Drug: Alvimopan|Drug: Alviompan Bowel Dysfunction|Constipation Cubist Pharmaceuticals LLC|GlaxoSmithKline August 2005 Phase 3
NCT00256932 Completed Drug: alvimopan|Drug: Placebo Bowel Dysfunction|Constipation Cubist Pharmaceuticals LLC|GlaxoSmithKline August 2005 Phase 3
NCT00241722 Completed Drug: Alvimopan|Drug: Placebo Bowel Dysfunction|Constipation Cubist Pharmaceuticals LLC|GlaxoSmithKline August 1 2005 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-11-29)

Tech Support

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