Discovery of CP-866,087, a mu opioid receptor antagonist for the treatment of alcohol abuse and dependence

CP-866,087 (compound 15) is a novel, potent and selective mu opioid receptor antagonist. The design rationale, synthesis, in vitro and in vivo biological evaluation are reported herein. Preclinical efficacy data in disease relevant models measuring reduction of alcohol intake are presented, along with preclinical pharmacokinetic properties which supported the selection of the title compound for clinical evaluation.