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U-47700 is a structural isomer of the earlier opioid AH-7921 and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold.
Upjohn looked for the key moieties which gave the greatest activity and posted over a dozen patents on related compounds, each optimizing one moiety] until they discovered that U-47700 was the most active.
U-47700 became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a single methylene spacer difference) and U-69,593, which share very similar structures. Although not used medically, the selective kappa ligands are used in research.