Acylmorphinans. A Novel Class of Potent Analgesic Agents

Article abstract of DOI:10.1021/jm00147a009

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.