On a black market, parafluorofentanyl is distributed in form of capsules and tablets containing the drug in the range of 33.8-408.7 ug. In preclinical studies parafluorofentanyl was administered to rats subcutaneously.

The potency of parafluorofentanyl with respect to cloned hMOR was investigated using the heterologous expression in X. laevis. Receptor subtype was individually coexpressed with GIRK1/GIRK2 channels and RGS4, mimicking the native neuronal G protein-mediated pathway of K1 channel activation. The two-microelectrode voltage-clamp technique was then used to measure the opioid receptor-activated GIRK1/GIRK2 channel response as the increase of the inward K1 current at 270 mV, evoked by the application of increasing concentrations of opioid ligands. Parafluorofentanyl activated hMOR with EC50 of 4.2 nM.