3-Hydroxy-17-aralkylmorphinans as potential opiate receptor-site-directed alkylating agents

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Abstract
To develop opiate receptor-site-directed alkylating agents, a series of 3-hydroxy-17-aralkylmorphinans containing reactive groups was synthesized and tested for analgesic and opiate antagonist activity in mice. Many of the target compounds exhibited agonistic characteristics; some were apparently active blockers of morphine analgesia. A more potent antagonist (41) [C28H30N2O3 .cntdot. HCl .cntdot. H2O.degree.] was investigated and its action was specifically associated with opiate receptors. Antagonist 41 could not be classified as a competitive or noncompetitive antagonist. The duration of 41 antagonist action in vivo and its in vitro receptor binding characteristics suggest that covalent association with opiate receptors is not an important factor.

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