Journal of Medicinal Chemistry p. 1775 - 1777 (1983)
Update date:2022-08-03
Topics:
Archer
Seyed-Mozaffari
Osei Gyimah
Bidlack
Abood
14β-(2-Bromoacetamido)morphine (6) and 14β-(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.
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