Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversibleμ-opioid receptorantagonist, with anIC₅₀of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor (K_i=0.47 nM) overκ-andδ-opioid receptors(K_is=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileus^[1][2][3].

IC50: 1.7 nM (μ-opioid receptor)^[1]

Alvimopan inhibits the loperamide-stimulated [³⁵S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC₅₀of 1.7 nM^[1].

Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of¹¹³Sn-labelled microspheres produced by morphine in rats^[3].
Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats^[3].

442.55

Solid

C₂₅H₃₄N₂O₅

1383577-62-5

爱维莫潘水合物

Room temperature in continental US; may vary elsewhere.