PT  - JOURNAL ARTICLE
AU  - John J. McGuire
AU  - Mahmoud Saifeddine
AU  - Chris R. Triggle
AU  - Kimberly Sun
AU  - Morley D. Hollenberg
TI  - 2-Furoyl-LIGRLO-amide: A Potent and Selective Proteinase-Activated Receptor 2 Agonist
AID  - 10.1124/jpet.103.064584
DP  - 2004 Jun 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 1124--1131
VI  - 309
IP  - 3
4099  - http://jpet.aspetjournals.org/content/309/3/1124.short
4100  - http://jpet.aspetjournals.org/content/309/3/1124.full
SO  - J Pharmacol Exp Ther2004 Jun 01; 309
AB  - A peptide corresponding to a proteinase-activated receptor 2 (PAR2)-activating peptide with an N-terminal furoyl group modification, 2-furoyl-LIGRLO-NH2, was assessed for PAR2-dependent and -independent biological activities. 2-Furoyl-LIGRLO-NH2 was 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-NH2 was 10 to 300 times more potent than SLIGRL-NH2. Unlike trans-cinnamoyl-LIGRLO-NH2, 2-furoyl-LI-GRLO-NH2 did not cause a prominent non-PAR2-mediated contraction of murine femoral arteries. In conclusion, 2-furoyl-LI-GRLO-NH2 represents the most potent and selective activator of PAR2 in biological systems described to date. The American Society for Pharmacology and Experimental Therapeutics