Journal of Medicinal Chemistry p. 1177 - 1180 (1985)
Update date:2022-08-04
Topics:
Mohacsi, Erno
O'Brien, Jay
Blount, John
Sepinwall, Jerry
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.
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