Document Report Card

ID: ALA1123025

Journal: J Med Chem

Title: Acylmorphinans. A novel class of potent analgesic agents.

Authors: Mohacsi E, O'Brien J, Blount J, Sepinwall J.

Abstract: A series of novel 2- and 3-acylmorphinans (8-14) was synthesized in our search for a potent analgesic agent with low addiction potential. The compounds were evaluated for antinociceptive potency and receptor binding affinity. Among these compounds, the levorotatory 3-acetyl-N-(cyclopropylmethyl)morphinan (12) was found to be an orally active analgesic, comparable in potency to morphine (1), yet only weakly able to substitute for morphine (1) in morphine-dependent rats.

CiteXplore: 2863378

DOI: 10.1021/jm00147a009