A K-opioid receptor agonist activates KOR in HEK293 cells expressing the human receptor (EC50 0 16 nM in a transactivation assay) inhibits forskolin-induced cAMP production in R1 G1 cells (EC50 0 048 nM) selective for KOR over MOR (EC50 1 UM in a transactivation assay) reduces acetic acid-induced writhing as well as GNTI-induced scratching behavior in mice (ED50s 0 07 and 0 05 mg/kg respectively)