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2-Furoyl-LIGRLO-amide is a potent and selective proteinase-activated receptor 2 (PAR2) agonist with a pD₂ value of 7.0..

Proteinase-activated receptor 2 (PAR2)

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.
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.

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.

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