Difelikefalin (trifluoroacetate salt)

Difelikefalin is a ?-opioid receptor (KOR) agonist.1It activates KOR in HEK293 cells expressing the human receptor (EC50= 0.16 nM in a transactivation assay) and inhibits forskolin-induced cAMP production in R1.G1 mouse thyoma cells (EC50= 0.048 nM) . Difelikefalin is selective for KOR over the ?-opioid receptor (MOR; EC50= >1 ?M in a transactivation assay) . It reduces acetic acid-induced writhing, as well as scratching behavior induced by the KOR antagonist GNTI, in mice (ED50s = 0.07 and 0.05 mg/kg, respectively) .