2-Furoyl-LIGRLO-amide TFA is a potent, selective agonist of the proteinase-activated receptor 2 (PAR2), with a pD2 value of 7.0 [1] [2].

2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH2) demonstrates equivalent efficacy and exhibits 10 to 25-fold greater potency than SLIGRLNH2 in elevating intracellular calcium levels in human and rat cells expressing PAR2, respectively [1]. In tissue, it surpasses SLIGRL-NH2 by 10 to 300 times in causing arterial vasodilation and hyperpolarization. Unlike trans-cinnamoyl-LIGRLO-NH2, it does not induce significant non-PAR2-mediated contraction in mouse femoral arteries [1].

When administered intradermally at the nape of the neck as a pre-injection at a dose of 10 μg, Furoyl-LIGRLO-amide TFA reduces scratching responses to 2-Furoyl-LIGRLO-amide in Trpv3 -/- mice, but not to histamine. In wild-type (WT) mice, however, the compound significantly decreases scratch behavior [3].