Alvimopan 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.
体内研究
Alvimopan (0.1-1.0 mg/kg; p.o.) partially antagonizes the slowing of small intestinal transit of 113 Sn-labelled microspheres produced by morphine 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.