Document Report Card

ID: ALA1122421

Journal: J Med Chem

Title: 14 beta-(2-bromoacetamido)morphine and 14 beta-(2-bromoacetamido)morphinone.

Authors: Archer S, Seyed-Mozaffari A, Osei-Gyimah P, Bidlack JM, Abood LG.

Abstract: 14 beta-(2-Bromoacetamido)morphine (6) and 14 beta-(2-bromoacetamido)morphinone (9) were prepared preferably from the adduct of thebaine and 1-chloro-1-nitrosocyclohexane, which on reduction in methanol solution gave 14-aminocodeinone (2) and the corresponding ketal (3). When tested in a receptor-binding assay, the IC50 values of 6 and 9 were 15 and 10 nM, respectively. If the incubation time during the assay was increased from 15 to 30 min, irreversible binding of both ligands was observed.

CiteXplore: 6315939

DOI: 10.1021/jm00366a024