Home Neuronal Signaling Opioid Receptor inhibitor Alvimopan dihydrate (LY246736 dihydrate) For research use only.

Alvimopan dihydrate (LY246736 dihydrate)

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) Chemical Structure

Alvimopan dihydrate (LY246736 dihydrate) Chemical Structure

CAS: 170098-38-1

Purity & Quality Control

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

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Signaling Pathway

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Opioid Receptor Signaling Pathway

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Biological Activity

Description 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.
Targets
μ-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(Ki) 40 nM(Ki)
In vitro
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 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].

Chemical Information & Solubility

Molecular Weight 460.56 Formula

C25H36N2O6
CAS No. 170098-38-1 SDF --
Smiles CC1CN(CCC1(C)C2=CC(=CC=C2)O)CC(CC3=CC=CC=C3)C(=O)NCC(=O)O.O.O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
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DMSO : 92 mg/mL ( (199.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)


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