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CARDIOVASCULAR
Canadian Institutes of Health Research Group on Regulation of Vascular Contractility, Smooth Muscle Research Group (J.J.M., C.R.T., M.D.H.) and Mucosal Inflammation Research Group (M.S., K.S., M.D.H.), Departments of Pharmacology & Therapeutics and Medicine, Faculty of Medicine, University of Calgary, Calgary, Alberta, Canada
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.
Address correspondence to: Dr. John J. McGuire, Cardiovascular Research Group, Division of Basic Medical Sciences, Faculty of Medicine, Memorial University of Newfoundland, St. John's, Newfoundland, Canada A1B 3V6. E-mail: mcguire{at}mun.ca
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