[2][3][4] U-47700 is a structural isomer of the earlier opioid AH-7921[6] and the result of a great deal of work elucidating the quantitative structure–activity relationship of the scaffold.

[16] U-47700 became the lead compound of selective kappa-opioid receptor ligands such as U-50488, U-51754 (containing a pyrrolidine rather than a dimethylamine substituent) and U-69,593, which share very similar structures.

[23][24] U-47700 has never been studied in humans, but it would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching and respiratory depression which could be harmful or fatal.

[47] U-47700 may be measured in serum, plasma, blood or urine to monitor for abuse, confirm a diagnosis of poisoning, or assist in a medicolegal death investigation.

Serum or blood U-47700 concentrations are expected to be in a range of 10–250 μg/L in intoxicated patients and 100–1,500 μg/L in deceased victims of acute overdosage.

[52] Responding to a perceived threat to public health and safety, the U.S. Drug Enforcement Administration has placed U-47700 into Schedule I of the Controlled Substances Act, effective November 14, 2016.