Description: Alvimopan (LY 246736) is a synthetic trans-3, 4-dimethyl-4-(3-hydroxyphenyl) piperidine with peripherally selective opioid mu receptor antagonist activity. Alvimopan is a selective and competitive antagonist at mu-opioid receptors, found in myenteric and submucosal neurons and the immune cells of the...

Alvimopan is a µ-opioid receptor antagonist (Ki = 0.47 nM). It is selective over the kappa- and delta-opioid receptors (Kis= 100 nM and 12 nM, respectively). Alvimopan inhibits µ-opioid receptor-mediated GTP binding to CHO cell membranes with an IC50 value of 1.7 nM. It inhibits morphine-induced slowing of...