Home Neuronal Signaling Opioid Receptor inhibitor Alvimopan dihydrate (LY246736 dihydrate)

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Alvimopan dihydrate (LY246736 dihydrate) Opioid Receptor inhibitor

Cat.No.S5701

Alvimopan (LY-246736) 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 dihydrate (LY246736 dihydrate) Opioid Receptor inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 460.56

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Quality Control

Batch: S570101 DMSO]92 mg/mL]false]]]false]]]false Purity: 99.05%
99.05

Solubility

In vitro
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DMSO : 92 mg/mL (199.75 mM)
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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 460.56 Formula

C25H36N2O6

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 170098-38-1 -- Storage of Stock Solutions

Synonyms N/A Smiles CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O.O.O

Mechanism of Action

Targets/IC50/Ki
μ-opioid receptor
(Cell-free assay)
0.77 nM(Ki)
δ-opioid receptor
(Cell-free assay)
4.4 nM(Ki)
κ-opioid receptor
(Cell-free assay)
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.
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.
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