Alvimopan monohydrate

Alvimopan monohydrate (ADL 8-2698 monohydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC 50 of 1.7 nM. Alvimopan monohydrate has selectivity for μ-opioid receptor ( K i =0.47 nM) over κ- and δ-opioid receptors ( K i s=100, 12 nM, respectively). Alvimopan monohydrate can be used for the research of postoperative ileusIn VitroAlvimopan inhibits the loperamide-stimulated [ 35 S]GTPγS binding to membranes containing the cloned human μ-opioid receptor, with an IC 50 of 1.7 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoAlvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113 Sn-labelled microspheres in rats. Alvimopan (3 mg/kg; p.o.) has no effect on the visceromotor behavioural responses (VMR) induced by noxious colorectal distension (CRD) in conscious rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only.Form:SolidIC50& Target:μ Opioid Receptor/MOR. Molecular Formula: C25H34N2O5 Molecular Weight: 442.5 PubChem CID: 71587995 Isomeric SMILES: C[C@H]1CN(CC[C@@]1(C)C2=CC(=CC=C2)O)C[C@H](CC3=CC=CC=C3)C(=O)NCC(=O)O.O