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Life Sciences | 1974

α-1-Acetylmethadol and its N-demethylated metabolites have potent opiate action in the guinea pig isolated ileum

Rodney Nickander; Richard N. Booher; Henry Miles

Abstract α-1-Acetylmethadol (LAM) and its N-demethylated metabolites α-1-noracetylmethadol (NAM) and α-1- dinoracetylmethadol (NNAM) exhibited opiate-like actions in vitro by depressing the electrically induced twitch of the longitudinal muscle of the guinea pig ileum. These effects were reversed by the opiate antagonist naloxone. The effect of both NAM and NNAM was approximately 15 times greater than LAM. The 50 percent inhibitory concentrations of the metabolites were well below those levels in plasma reported for man. The long duration of action of LAM as an opiate substitute is most likely due to the conversion to its metabolites.


Journal of Medicinal Chemistry | 1973

Metabolism of acetylmethadol. A sensitive assay for noracetylmethadol and the identification of a new active metabolite.

Ruth E. Billings; Richard N. Booher; Stephen E. Smits; Albert Pohland; Robert E. McMahon


Journal of Organic Chemistry | 1997

Application of Palladium(0)-Catalyzed Processes to the Synthesis of Oxazole-Containing Partial Ergot Alkaloids

Benjamin Alan Anderson; Lisa M. Becke; Richard N. Booher; Michael Edward Flaugh; Nancy Kay Harn; Thomas J. Kress; David L. Varie; James P. Wepsiec


Archive | 1995

6-heterocyclic-4-amino-1,2,2A,3,4,5-hexahydrobenz[cd]indoles

Richard N. Booher; David Ernest Lawhorn; Michael J. Martinelli; Charles J. Paget; John Mehnert Schaus


Archive | 1995

6-heterocyclic-4-amino-1,3,4,5-tetrahydrobenz[CD] indoles

Richard N. Booher; David Ernest Lawhorn; Charles J. Paget; John Mehnert Schaus


Journal of Medicinal Chemistry | 1987

Synthesis of D-oxa tricyclic partial ergolines as dopamine agonists

Richard N. Booher; Edmund C. Kornfeld; E. Barry Smalstig; James A. Clemens


Journal of Medicinal Chemistry | 1977

Various 5-substituted and 2,5-disubstituted 1,3-dioxanes, a new class of analgesic agents.

Richard N. Booher; Stephen E. Smits; William W. Turner; Albert Pohland


Journal of Medicinal Chemistry | 1975

Synthesis of a new metabolite of acetylmethadol.

Richard N. Booher; Albert Pohland


Journal of Medicinal Chemistry | 1977

Synthesis of two metabolites of (+)-propoxyphene

William W. Turner; Richard N. Booher; Stephen E. Smits; Albert Pohland


Archive | 1991

6-HETEROCYCLIC-4-AMINO-1,2,2A,3,4,5-HEXAHYDROBENZ(CD)INDOLES AND PHARMACEUTICAL USE THEREOF

Richard N. Booher; David Ernest Lawhorn; Michael J. Martinelli; Charles J. Paget; John Mehnert Schaus

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