Proteinase-activated receptor 2 (PAR2)
2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH 2 ) is equally effective to and 10 to 25 times more potent than SLIGRLNH 2 for increasing intracellular calcium in cultured human and rat PAR2-expressing cells, respectively. In bioassays of tissue PAR2 activity, measured as arterial vasodilation and hyperpolarization, 2-Furoyl-LIGRLO-amide (2-Furoyl-LIGRLO-NH 2 ) is 10 to 300 times more potent than SLIGRL-NH 2 . Unlike trans-cinnamoyl-LIGRLO-NH 2 , 2-Furoyl-LIGRLO-amide do not cause a prominent non-PAR2-mediated contraction of murine femoral arteries.
Furoyl-LIGRLO-amide (injected intradermally at the nape of the neck; 10 μg; pre-injected) exhibits fewer scratches in response to 2-Furoyl-LIGRLO-amide but not to histamine in Trpv3 -/- mice. But it decreases significantly the number of scratches in WT mice.