The peptide 2-furoyl-LIGRLO-NH2 showed higher potency and receptor selectivity for in vitro assays than other PAR-2-activating peptides. 2-Furoyl-LIGRLO-NH2 peptide was equally or more potent than SLIGRL-NH2 for increasing intracellular calcium in cultured human and rat PAR-2-expressing cells and significantly more potent than SLIGRL-NH2 in assays of tissue PAR-2 activity.