2-Furoyl-LIGRLO-amide TFA is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD2 value of 7.0[1][2]..
2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) is equally effective to and 10 to 25 times more potent than SLIGRLNH2 for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively[1]. In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) is 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries[1].
[1]. McGuire JJ, et al. 2-furoyl-LIGRLO-amide: a potent and selective proteinase-activated receptor 2 agonist. J Pharmacol Exp Ther. 2004 Jun;309(3):1124-31. [2]. Lohman RJ, et al. An antagonist of human protease activated receptor-2 attenuates PAR2 signaling, macrophage activation, mast cell degranulation, and collagen-induced arthritis in rats. FASEB J. 2012 Jul;26(7):2877-87.